Publications

1. Harold Kohn, Stephen J. Benkovic,* and R.A. Olofson,* Dependence of Mechanism on pH for Deuterium-Hydrogen Exchange in 1-Methyltetrazole-5-d.  Transition Metal Ion Catalysis of a Deprotonation Process, J. Am. Chem. Soc., 94, 5759-5765 (1972).

2. Harold Kohn and R.A. Olofson,* 1, 4-Dimethyl-1, 4-dihydro-1, 2, 4, 5-tetrazine and Its N-Alkyl Salt.  Synthesis, Structure and Chemistry. J. Org. Chem., 37, 3504-3509 (1972).

3. Ronald Breslow,* Harold Kohn, and Brock Siegel, Methylated Cyclodextrin and a Cyclodextrin Polymer as Catalysts in Selective Anisole Chlorination, Tetrahedron Lett., 17, 1645-1646 (1976).

4. Harold Kohn,* Model Studies on the Mechanism of Biotin Department Carboxylations, J. Am. Chem. Soc., 98, 3690-3694 (1976).

5. Harold Kohn* and Y. Gopichand, An Isosteric Substitution Reaction of Substituted Imidazolidinethiones, Tetrahedron Lett., 17, 3093-3096 (1976).

6. Harold Kohn* and Raymond E. Davis, Syntheses and Chemistry of N-Acyl Substituted Dihydroimidazo[2, 1-b]thiazolium Salts, J. Org. Chem., 42, 72-77 (1977).

7. Harold Kohn,* Melanie J. Cravey, Janice H. Arceneaux, Rodney L. Cravey, and M. R. Willcott, III, Syntheses and Spectral Properties of Substituted Imidazolidones and Imidazolines, J. Org. Chem., 42, 941-948 (1977).

8. Harold Kohn* and Janice H. Arceneaux, Thermolysis of N-Acyl Substituted 2-Allylthioimidazolines.  Evidence for a [3,3] Sigmatropic Rearrangement, J. Org. Chem., 42, 2339-2341 (1977).

9. Harold Kohn,* Barbara A. Kohn, Marie Louise Steenberg, and Joseph P. Buckley, Syntheses and Pharmacological Activity of Substituted Imidazolidinethiones and Thioimidazolines, J. Med. Chem., 20, 158-160 (1977).

10. Steven F. Watkins,* Harold Kohn,* and Ivan Bernal, Crystal and Molecular Structure of Methyl 3-Methyl-2-thioxoimidazolidine-1-carboxylate.  A Possible Structural Analogue for Caboxybiotin, J. Chem. Soc., Perkin Trans. II, 26-29 (1978).

11. Janice H. Arceneaux, Harold Kohn,* Marie Louise Steenberg, and Joseph P. Buckley,* Synthesis and Pharmacological Activity of N-Acyl-substituted Imidazolidinethiones and Thioimidazolines, J. Pharm. Sci., 67, 600-602 (1978).

12. Harold Kohn,* Y. Gopichand, and P. Charumilind, Studies on the Reaction of Acylimidazolidones with Ketenes, J. Org. Chem., 43, 4955-4961 (1978).

13. Harold Kohn,* P. Charumilind, and Y. Gopichand, Studies on the Reaction of Thiocarbonyl-Containing Compounds with Ketenes, J. Org. Chem., 43, 4961-4965 (1978).

14. Christian von Rohrscheidt and Harold Kohn,* Selective Formation and Hydrolysis of Derivatives of 4-lodo-3-ureido-1-butanol, Tetrahedron Lett., 215-218 (1979).

15. Harold Kohn,* P. Charumilind, and S.H. Simonsen, 3,3,4,4-Tetraphenyl-1, 2-oxathiolan-5-one 2-Oxide.  Synthesis, Structure and Selected Chemistry, J. Am. Chem. Soc., 101, 5431-5432 (1979).

16. Melanie J. Cravey and Harold Kohn,* Model Studies on the Mechanism of Biotin-Dependent Carboxylations. 2. Site of Protonation vs. CO2-Transfer, J. Am. Chem. Soc., 102, 3928-3939 (1980).

17. P. Charumilind and Harold Kohn,* Studies on the Reaction of 3,3,4,4-Tetraphenylthietan-2-one, J. Org. Chem., 45, 4359-4365 (1980).

18. Harry Flaster and Harold Kohn,* Syntheses and Spectral Properties of 2-Thiobiotin and Biotin Derivatives, J. Heterocyclic Chem., 18, 1425-1436 (1981).

19. Harold Kohn,* Mary B. Bean, Christian von Rohrscheidt, M. R. Willcott, III, and E. W. Warnhoff, Participation in the Formation of lodo Ureas from 3-Buten-1-ol Derivatives.  A Reinvestigation, Tetrahedron, 37, 3195-3201 (1981).

20. Harold Kohn* and Zeng-Kun Liao, N-Amidoyliminium Ion Cyclizations.  Synthesis of Annelated Imidazolidinones, J. Org. Chem., 47, 2787-2789 (1982).

21. Sergio Cortes and Harold Kohn,* Selective Reductions of 3-Substituted Hydantoins to 4-Hydroxy-2-imidazolidinones and Vicinal Diamines, J. Org. Chem., 48, 2246-2254 (1983).

22. I.-Ching Chiu and Harold Kohn,* Synthesis and Reactivity of trans-6-Azabicyclo[3.1.0]hexan-2-ol Derivatives and Indano[1, 2-b]aziridine.  Structural Analogues of Mitomycin C., J. Org. Chem., 48, 2857-2866 (1983).

23. Mary Bean and Harold Kohn,* Studies on the Reaction of Mitomycin C with Potassium Ethyl Monothiocarbonate under Reductive Conditions, J. Org. Chem., 48, 5033-5041 (1983).

24. Ulfert Hornemann,* Kazuo Iguchi, Paul J. Keller, Huynh M. Vu, John F. Kozlowski, and Harold Kohn,* Reactions of Mitomycin C with Potassium Ethyl Xanthate in Neutral Aqueous Solution, J. Org. Chem., 48, 5026-5033 (1983).

25. Harold Kohn* and Sang-Hun Jung, New Stereoselective Method for the Preparation of Vicinal Diamines from Olefins and Cyanamide, J. Am. Chem. Soc., 105, 4106-4108 (1983).

26. Harold Kohn* and Nada Zein, Studies Concerning the Mechanism of Electrophilic Substitution Reactions of Mitomycin C, J. Am. Chem. Soc., 105, 4105-4106 (1983).

27. Sang-Hun Jung and Harold Kohn,* A New Reductive Procedure for the Preparation of Vicinal Diamines and Monoamines, Tetrahedron Lett., 25, 399-402 (1984).

28. Zeng-Kun Liao and Harold Kohn,* Intramolecular N-Carbamoyliminium Ion Cyclizations of Unactivated Alkenes and Acetylenes, J. Org. Chem., 49, 3812-3819 (1984).

29. Zeng-Kun Liao and Harold Kohn,* Synthesis of Substituted 2-Imidazolidinones and Annelated Hydantoins via Amidoalkylation Transformations, J. Org. Chem., 49, 4745-4752 (1984).

30. Sergio Cortes, Zeng-Kun Liao, Darrell Watson, and Harold Kohn,* The Effect of Structural Modification of the Hydantoin Ring on Anticonvulsant Activity, J. Med. Chem., 28, 601-606 (1985).

31. Mary Bean and Harold Kohn,* Studies on the Reaction of Mitomycin C with Potassium Thiobenzoate under Reductive Conditions, J. Org. Chem., 50, 293-298 (1985).

32. Sang-Hun Jung and Harold Kohn,* Stereoselective Synthesis of Vicinal Diamines from Alkenes and Cyanamide, J. Am. Chem. Soc., 107, 2931-2943 (1985).

33. Zeng-Kun Liao and Harold Kohn,* Synthesis of Spiroimidazolidin-2-ones via Intramolecular N-Carbamoyliminium Ion Cyclization Reactions, J. Org. Chem., 50, 1884-1888 (1985).

34. Sang-Hun Jung and Harold Kohn,* The Chemical Reactivity of Ethyl 2,2,3,3-Tetramethyl-1-aziridinecarboximidate, Heterocycles, 23, 2045-2050 (1985).

35. Nada Zein and Harold Kohn,* The Electrophilic and Nucleophilic Character of the Carbon-10 Methylene Group in Mitosenes Revealed, J. Am. Chem. Soc., 108, 296-297 (1986).

36. Harold Kohn,* Nada Zein, X. Q. Lin, J.-Q. Ding, and K.M. Kadish,* Mechanistic Studies on the Mode of Reaction of Mitomycin C under Catalytic and Electrochemical Reductive Conditions, J. Am. Chem. Soc., 109, 1833-1840 (1987).

37. Nada Zein and Harold Kohn,* Covalent Binding of Mitomycin C to Nucleosides under Reductive Conditions, J. Am. Chem. Soc., 109, 1576-1577 (1987).

38. Judith D. Conley and Harold Kohn,* Functionalized DL-Amino Acid Derivatives.  Potent New Agents for the Treatment of Epilepsy, J. Med. Chem., 30, 567-574 (1987).

39. Nim Ming Nguy, I.-Ching Chiu, and Harold Kohn,* Synthesis and Reactivity of 6- and 7-Methoxyindano[1,2-b]aziridines, J. Org. Chem., 52, 1649-1655 (1987).

40. Paul L. Fishbein and Harold Kohn,* Synthesis and Antineoplastic Activity of (N)-la-Formyl and (N)-la-Thionoformyl Derivatives of Mitomycin C and (N)-2-Methylaziridine, J. Med. Chem., 30, 1767-1773 (1987).

41. Harold Kohn* and Judith D. Conley, New Antiepileptic Agents, Chemistry in Britain, 24, 231-234 (1988).

42. Harold Kohn* and Syed Abuzar, Reinterpretation of the Bicyclomycin-Sodium Methanethiolate Reaction, J. Am. Chem. Soc., 110, 3661-3663 (1988).

43. Harold  Kohn,* Syed Abuzar, James D. Korp, Andrew S. Zektzer, and Gary E. Martin,* Structural Studies of Bicyclomycin, J. Heterocyclic Chem., 25, 1511-1517 (1988).

44. Harold Kohn* and Syed Abuzar, Studies on the Chemical Reactivity of Bicyclomycin:  Acid Hydrolysis, J. Org. Chem., 53, 2769-2773 (1988).

45. Harold Kohn,* Judith D. Conley, and J. David Leander,* Marked Stereospecificity in a New Class of Anticonvulsants, Brain Research, 457, 371-375 (1988).

46. Philippe LeGall, Kailash N. Sawhney, Judith D. Conley, and Harold Kohn,* Synthesis of Functionalized Non-natural Amino Acid Derivatives via Amidoalkylation Transformations, Int. J. Peptide Protein Res., 32, 279-291 (1988).

47. Syed Abuzar and Harold Kohn,* Observations on the Activation of Bicyclomycin, J. Am. Chem. Soc., 110, 4089-4090 (1988).

48. C. H. Lee and Harold Kohn,* 3,7-Bis(carboethoxy)perhydro-1,5,2,4,6,8-dithiatetrazocine 1,1,5,5-Tetroxide.  Synthesis, Structure, and Chemistry, Heterocycles, 27, 2581-2588 (1988).

49. Kailash N. Sawhney and Harold Kohn,* Mitomycin C Analogues with a Substituted Hydrazine at Position 7.  Synthesis, Spectral Properties, and Biological Activity, J. Med. Chem., 32, 248-252 (1989).

50. Syed Abuzar and Harold Kohn,* Studies on the Reactivity of Bicyclomycin with Amines, J. Am. Chem. Soc., 111, 4895-4903 (1989).

51. C. H. Lee, James D. Korp, and Harold Kohn,* 3-Oxo- and 3-Imino-4-substituted-1,2,5-thiadiazolidine 1, 1-Dioxides.  Synthesis, Spectral Properties, and Selected Chemistry, J. Org. Chem., 54, 3077-3083 (1989).

52. Syed Abuzar and Harold Kohn,* Studies on the Reactivity of Bicyclomycin with Nucleophilic Amino Acid Derivatives, J. Org. Chem., 54, 4000-4003 (1989).

53. David J. Russell and Harold Kohn,* Development of a Hydrazine-mediated System for the Reductive Activation of Mitomycin C, Heterocycles, 31, 223-227 (1990).

54. C. H. Lee and Harold Kohn,* Anticonvulsant Properties of 3-Oxo- and 3-Imino-4-substituted-1,2,5-thiadiazolidine 1,1-Dioxides, J. Pharm. Sci., 79, 716-718 (1990).

55. Harold Kohn,* Kailash N. Sawhney, Philippe LeGall, Judith D. Conley, David W. Robertson, and J. David Leander, Preparation and Anticonvulsant Activity of a Series of Functionalized -Aromatic and -Heteroaromatic Amino Acids, J. Med. Chem., 33, 919-926 (1990).

56. Syed Abuzar and Harold Kohn,* Studies on the Reactivity of the Bicyclomycin with Thiols, J. Am. Chem. Soc., 112, 3114-3121 (1990).

57. Harold Kohn* and Y. Hong, Observations on the Activation of Mitomycin C. Requirements for C-10 Functionalization, J. Am. Chem. Soc., 112, 4596-4598 (1990).

58. Chai-Ho Lee and Harold Kohn,* Intra- and Intermolecular -Sulfamidoalkylation Reactions, J. Org. Chem., 55, 6098-6104 (1990).

59. Chai-Ho Lee and Harold Kohn,* Functionalized 5,6-Dihydro-2H-1,2,6-Thiadiazine 1,1-Dioxides.  Synthesis, Structure and Chemistry, J. Heterocyclic Chem., 27, 2107-2111 (1990).

60. Ven-Shun Li and Harold Kohn,* Studies on the Bonding Specificity for Mitomycin-DNA Monoalkylation Processes, J. Am. Chem. Soc., 113, 275-283 (1991).

61. Y. P. Hong and Harold Kohn,* Studies on the Use of Cr(ClO4)2 for the Reductive Activation of Mitomycin C, J. Am. Chem. Soc., 113, 4634-4644 (1991).

62. Insook Han and Harold Kohn,* 7-Aminoaziridinomitosenes:  Synthesis, Structure, and Chemistry, J. Org. Chem., 56, 4648-4653 (1991).

63. Harold Kohn,* Kailash N. Sawhney, Philippe LeGall, David W. Robertson, and J. David Leander, Preparation and Anticonvulsant Activity of a Series of Functionalized -Heteroatom Substituted Amino Acids, J. Med. Chem., 34, 2444-2452 (1991).

64. Marco A. Vela and Harold Kohn,* Studies on the Reactivity of Bicyclomycin 3'-O-Methanesulfonate.  A Novel Ring-Expansion Transformation, J. Org. Chem., 56, 5462-5464 (1991).

65. Y. P. Hong and Harold Kohn,* Cr(ClO4)2:  An Effective Reagent for the Preparation of Mitomycin C Nucleophilic Substituted Compounds, J. Org. Chem., 56, 6479-6482 (1991).

66. Insook Han, David J. Russell, and Harold Kohn,* Studies on the Mechanism of Mitomycin C(1)-Electrophilic Transformations:  Structure-Reactivity Relationships, J. Org. Chem., 57, 1799-1807 (1992).

67. Harold Kohn,* Ven-Shun Li, and Moon-shong Tang,* Recognition of Mitomycin C-DNA Monoadducts by UVRABC Nuclease, J. Am. Chem. Soc., 114, 5501-5509 (1992).

68. Yeong Soo Oh and Harold Kohn,* Comparative Studies on the Reactivity of 4-Methylene-1-oxa-6,9-diazaspiro[4.5]decane-7,10-dione, 1-Acetyl-3-hydroxy-3-vinyl-2,5-piperazinedione, and Bicyclomycin.  Examination of a Key Structural Element Necessary for Bicyclomycin-mediated Transformations, J. Org. Chem., 57, 3662-3672 (1992).

69. Pascal Schiltz and Harold Kohn,* Sodium Dithionite-Mediated Mitomycin C Reductive Activation Processes, Tetrahedron Lett., 33, 4709-4712 (1992).

70. Marco A. Vela and Harold Kohn,* The Synthesis and Reactivity of [N(8)-C(3')]-Cyclized Bicyclomycin.  Evidence of the Role of the C(1)-Triol Group in Bicyclomycin-Mediated Processes, J. Org. Chem., 57, 5223-5231 (1992).

71. Pascal Schiltz and Harold Kohn,* Reductively Activated Mitomycin C:  An Efficient Trapping Reagent for Electrophiles, J. Am. Chem. Soc., 114, 7958-7959 (1992).

72. Marco A. Vela and Harold Kohn,* Observations Concerning the Reactivity of Bicyclomycin and Bicyclomycin Derivatives with Organophosphorous Reagents, J. Org. Chem., 57, 6650-6653 (1992).

73. Harold Kohn,* Ven-Shun Li, Pascal Schiltz, and Moon-shong Tang,* On the Origins of the DNA Sequence Selectivity of Mitomycin Monoalkylation Transformations, J. Am. Chem. Soc., 114, 9218-9220 (1992).

74. Harold Kohn,* Ven-Shun Li, Pascal Schiltz, and Moon-shong Tang, Studies Concerning the Origins of the Selectivity of Mitomycin-DNA Monoalkylation Transformations, Verlag Helv. Chim. Acta (Proceedings of the XIIth International Symposium on Medicinal Chemistry), pp. 331-346 (1993).

75. Antoni Zwiefka, Harold Kohn,* and William R. Widger,* Transcription Termination Factor rho:  The Site of Bicyclomycin Inhibition in Escherichia coli, Biochemistry, 32, 3564-3570 (1993).

76. Pascal Schiltz and Harold Kohn*, Studies on the Use of Na2S2O4 for the Reductive Activation of Mitomycin C, J. Am. Chem. Soc., 115, 10497-10509 (1993).

77. Pascal Schiltz and Harold Kohn,* Studies on the Reactivity of Reductively Activated Mitomycin C, J. Am. Chem. Soc., 115, 10510-10518 (1993).

78. Suganthini Subramaniam and Harold Kohn,* Comparative Reactivities of Mitomycin C, 7-(N-Piperidino)mitomycin, and Mitomycin A.  The Role of the C(7) Substituent, J. Am. Chem. Soc., 115, 10519-10526 (1993).

79. Harold Kohn,* Kailash N. Sawhney, Patrick Bardel, David W. Robertson and J. David Leander, Synthesis and Anticonvulsant Activities of -Heterocyclic -Acetamido-N-benzylacetamide Derivatives, J. Med. Chem., 36, 3350-3360 (1993).

80. Harold Kohn,* Kailash N. Sawhney, David W. Robertson, and J. David Leander, Anticonvulsant Properties of N-Substituted ,-Diamino Acid Derivatives, J. Pharm. Sci., 83, 689-691 (1994).

81. Hyeung-geun Park, Marco A. Vela, and Harold Kohn,* Synthesis and Reactivity of Bicyclomycin C(3') Amines, J. Am. Chem. Soc., 116, 471-478 (1994).

82. Zhuming Zhang and Harold Kohn,* The Role of the C(1) Triol Group in Bicyclomycin, J.C.S. Chem. Commun., 1343-1344 (1994).

83. Zhuming Zhang, and Harold Kohn,* Chemical, Biochemical, and Biological Studies of Select C(1) Triol Modified Bicyclomycins, J. Am. Chem. Soc., 116, 9815-9826 (1994).

84. Patrick Bardel, Antoinette Bolanos, and Harold Kohn,* Synthesis and Anticonvulsant Activities of -Acetamido-N-benzylacetamide Derivatives Containing an Electron-deficient -Heteroaromatic Substituent, J. Med. Chem., 37, 4567-4571 (1994).

85. Hyeung-geun Park, Antoni Zwiefka, William Widger,* and Harold Kohn,* Bicyclomycin and Dihydrobicyclomycin Inhibition Kinetics of Escherichia coli rho-Dependent Transcription Termination Factor ATPase Activity, Arch. Biochem. Biophys., 323, 447-454 (1995).

86. Ven-Shun Li, Daeock Choi, Moon-shong Tang,* and Harold Kohn,* Structural Requirements for Mitomycin C DNA Bonding, Biochemistry, 34, 7120-7126 (1995).

87. Daeock Choi, Byungwoo Yoo, Kimberly L. Colson, Gary E. Martin, and Harold Kohn,* C(10) Halogen 10-Deoxycarbamoylporfiromycins:  Synthesis, Chemistry, and Biological Activity, J. Org. Chem., 60, 3391-3396 (1995).

88. Zhuming Zhang, Hyeung-guen Park, and Harold Kohn,* Bicyclomycin Oxidative Transformations.  Synthesis and Properties of Bicyclomycin-5-norketone, J. Org. Chem., 60, 5346-5351 (1995).

89. Daeock Choi and Harold Kohn,* Trimethylsilyl Halides:  Effective Reagents for the Synthesis of β-Halo Amino Acid Derivatives, Tetrahedron Lett., 36, 7011-7014 (1995).

90. Daeock Choi and Harold Kohn,* Expedient Syntheses of Racemic 2,3-Diaminopropanoic Acid Derivatives, Tetrahedron Lett., 36, 7371-7374 (1995).

91. Alejandro Santillán, Jr. and Harold Kohn,* Novel Ring Transformations for 5,5a-Dibromobicyclomycin and Derivatives, Tetrahedron, 52, 833-842 (1996).

92. Ven-Shun Li, Daeock Choi, Zheng Wang, Leslie S. Jimenez, Moon-shong Tang,* and Harold Kohn,* Role of the C-10 Substituent in Mitomycin C-1—DNA Bonding, J. Am. Chem. Soc., 118, 2326-2331 (1996).

93. Ven-Shun Li, Daeock Choi, Moon-shong Tang, and Harold Kohn,* Concerning In Vitro Mitomycin—DNA Alkylation, J. Am. Chem. Soc., 118, 3765-3766 (1996). 

94. Daeock Choi, James P. Stables, and Harold Kohn,* Synthesis and Anticonvulsant Activities of N -Benzyl 2-Acetamidopropionamide Derivatives, J. Med. Chem., 39, 1907-1916 (1996).

95. Harold Kohn* and Shuang Wang, Studies on the Mechanism of Activation of C(7) Ethylenediamine Substituted Mitomycins.  Relevance to the Proposed Mode of Action of BMY-25067 and KW-2149, Tetrahedron Lett., 37, 2337-2340 (1996).

96. Attila Magyar, Xiangdong Zhang, Harold Kohn,* and William R. Widger,* The Antibiotic Bicyclomycin Affects the Secondary RNA Binding Site of Escherichia coli Transcription Termination Factor Rho, J. Biol. Chem., 271, 25369-25374 (1996).

97. Daeock Choi, James P. Stables, and Harold Kohn,* The Anticonvulsant Activities of Functionalized N-Benzyl 2-Acetamidoacetamides.  The Importance of the 2-Acetamido Substituent, Bioorg. Med. Chem., 4, 2105-2114 (1996).

98. Hyeung-geun Park, Xiangdong Zhang, William R. Widger, and Harold Kohn,* The Role of the C(1) Triol Group in Bicyclomycin:  Synthesis and Biochemical and Biological Properties, J. Org. Chem., 61, 7750-7755 (1996).

99. Alejandro Santillán, Jr., Hyeung-geun Park, Xiangdong Zhang, Oh-Seuk Lee, William R. Widger, and Harold Kohn,* The Role of the [4.2.2] Bicyclic Unit in Bicyclomycin:  Synthesis, Structure, Chemical, Biochemical, and Biological Properties, J. Org. Chem., 61, 7756-7763 (1996).

100. Hyeung-geun Park, Zhuming Zhang, Xiangdong Zhang, William R. Widger, and Harold Kohn,* The Role of the C(5)-C(5a) Exomethylene Group in Bicyclomycin:  Synthesis, Structure, and Biochemical and Biological Properties, J. Org. Chem., 61, 7764-7776 (1996).

101. Nam Huh, Ajay A. Rege, Byungwoo Yoo, Timothy P. Kogan,* and Harold Kohn,* Design, Synthesis, and Evaluation of Mitomycin-tethered Antisense Agents, Bioconj. Chem., 7, 659-669 (1996).

102. Shuang Wang and Harold Kohn,* Mitomycin Betaines:  Synthesis, Structure, and Reactivity, J. Org. Chem., 61, 9202-9206 (1996).

103. Nam Huh, Timothy P. Kogan,* and Harold Kohn,* Synthesis of N-Substituted 10-Des(carbamoyloxy)-10-azidomitomycins, Synthesis, 921-924 (1997).

104. Shuang Wang and Harold Kohn,* C(7)-Substituted Diaminomitomycins:  Synthesis, Structure, and Chemical Reactivity, J. Org. Chem., 62, 5404-5412 (1997).

105. Hangjin Cho, Hyeung-geun Park, Xiangdong Zhang, Isabel Riba, Simon J. Gaskell, William R. Widger,* and Harold Kohn,* Design, Syntheses, and Evaluations of Bicyclomycin-Based Rho Inactivators, J. Org. Chem., 62, 5432-5440 (1997).

106. Alejandro Santillán, Jr., Xiangdong Zhang, William R. Widger, and Harold Kohn,* 5a-Methyl-substituted Bicyclomycins:  Synthesis, Chemical, Biochemical and Biological Properties, J. Org. Chem., 63, 1290-1298 (1998). 

107. Alejandro Santillán, Jr., Xiangdong Zhang, Jon Hardesty, William R. Widger, and Harold Kohn,* Role of the C(6) Hydroxy Group in Bicyclomycin:  Synthesis, Structure, Chemical, Biochemical and Biological Properties, J. Med. Chem., 41, 1185-1194 (1998).

108. Isabel Riba, Simon J. Gaskell,* Hangjin Cho, William R. Widger, and Harold Kohn,* Evidence for the Location of Bicyclomycin Binding to the Escherichia coli Transcription Termination Factor Rho, J. Biol. Chem., 273, 34033-34041 (1998).

109. Shridhar V. Andurkar, James P. Stables, and Harold Kohn,* Synthesis and Anticonvulsant Activities of (R)-(O)-Methylserine Derivatives, Tetrahedron:  Asymmetry, 9, 3841-3854 (1998).

110. Attila Magyar, Xiangdong Zhang, Fadi Abdi, Harold Kohn,* and William R. Widger,* Identifying the Bicyclomycin Binding Domain through Biochemical Analysis of Antibiotic-Resistant Rho Proteins, J. Biol. Chem., 274, 7316-7324 (1999).

111. Shridhar V. Andurkar, James P. Stables, and Harold Kohn,* The Anticonvulsant Activities of N -Benzyl 3-Methoxypropionamides, Bioorg. Med. Chem., 7, 2381-2389 (1999).

112. Shuang Wang, and Harold Kohn,* Studies on the Mode of Action of BMS-181174 and KW-2149:  The Reactivity of 7-N-(Mercaptoethyl)mitomycin C, J. Med. Chem., 42, 788-790 (1999).

113. Ven-Shin Li, Matthew Reed, Yi Zheng, Harold Kohn,* and Moon-shong Tang,* C5 Cytosine Methylation at CpG Sites Enhances Sequence Selectivity of Mitomycin C-DNA Bonding, Biochemistry, 39, 2612-2618 (2000).

114. Chen Wang and Harold Kohn,* Formation of Aromatic Rings through Enamine Annulation, Organic Letters 2, 1773-1775 (2000).

115. Fabien Vincent, William R. Widger,* Matthew Openshaw, Simon J. Gaskell, and Harold Kohn,* 5a-Formylbicyclomycin:  Studies on the Bicyclomycin-Rho Interaction, Biochemistry, 39, 9067-9076 (2000).

116. Fabien Vincent, Matthew Openshaw, Mark Trautwein, Simon J. Gaskell,* Harold Kohn,* and William R. Widger,* Rho Transcription Factor:  Symmetry and Binding of Bicyclomycin, Biochemistry, 39, 9077-9083 (2000).

117. Ven-Shun Li, Moon-shong Tang,* and Harold Kohn,* The Effect of C(5) Cytosine Methylation at   CpG Sequences on Mitomycin-DNA Bonding Profiles, Bioorg. Med. Chem., 9, 863-873 (2001).

118. Fabien Vincent, Jayasree Srinivansan, Alejandro Santillán, Jr., William R. Widger,* and Harold Kohn,* C(5)-C(5a)-Modified Bicyclomycins:  Synthesis, Structure, and Biochemical and Biological Properties, J. Org. Chem., 66, 2251-2264 (2001).

119. Shridhar V. Andurkar, Cécile Béguin, J. P. Stables, and Harold Kohn,* Synthesis and Structural Studies of Aza Analogues of Functionalized Amino Acids:  New Anticonvulsant Agents, J. Med. Chem., 44, 1475-1478 (2001).

120. Younghwa Na and Harold Kohn,* Quinone-Cyclized Porfiromycins, Heterocycles, 55, 1347-1363 (2001).

121. Arnaud LeTiran, James P. Stables, and Harold Kohn,* Functionalized Amino Acid Anticonvulsants.  Synthesis and Pharmacological Evaluation of Conformationally Restricted Analogues, Bioorg. Med. Chem., 9, 2693-2708 (2001).

122. Maha Zewail-Foote, Ven-Shun Li, Harold Kohn, David Bearss, Mary Guzman, and Laurence H. Hurley,* The Pattern of Ecteinascidin 743-DNA Adducts by the UvrABC Nuclease and the Unique Structural Feature of the DNA Adducts Can Be Used to Explain the Repair-Dependent Toxicities of this Antitumor Agent, Chem. and Biol., 8, 1033-1049 (2001).

123. Younghwa Na, Ven-Shun Li, Yuka Nakanishi, Kenneth F. Bastow, and Harold Kohn,* Synthesis, DNA Cross-linking Activity, and Cytotoxicity of Dimeric Mitomycins, J. Med. Chem., 44, 3453-3462 (2001).

124. Sang Hyup Lee and Harold Kohn,* Efficient Synthesis of Medium-sized Cyclic Ether Diamines, J. Org. Chem., 67, 1692-1695 (2002).

125. Min Shen, Arnaud LeTiran, Yunde Xiao, Alexander Golbraikh, Harold Kohn,* and Alexander Tropsha,* Quantitative Structure-Activity Relationship Analysis of Functionalized Amino Acid Anticonvulsant Agents Using k Nearest Neighbor and Simulated Annealing PLS Methods, J. Med. Chem., 45, 2811-2823 (2002).

126. Younghwa Na, Shuang Wang, and Harold Kohn,* 7-N-(Mercaptoalkyl)mitomycins:  Implications of Cyclization for Drug Function, J. Am. Chem. Soc., 124, 4666-4677 (2002).

127. Yi Xu, Harold Kohn, and William R. Widger,* Mutations in the Rho Transcription Termination Factor That Affect RNA Tracking, J. Biol. Chem., 277, 30023-30030 (2002).

128. Arnaud LeTiran, James P. Stables, and Harold Kohn,* Design and Evaluation of Affinity Labels of Functionalized Amino Acid Anticonvulsants, J. Med. Chem., 45, 4762-4773 (2002).

129. Thomas P. Weber, William R. Widger,* and Harold Kohn,* The Mg2+ Requirements for Rho Transcription Termination Factor:  Catalysis and Bicyclomycin Inhibition, Biochemistry, 41, 12377-12383 (2002).

130. Sang Hyup Lee and Harold Kohn,* Phosphine-Assisted Rearrangement of 4,5-Dihydroxy-1,2-Dithianes to 4-Hydroxy-3-Mercaptotetrahydrothiophenes, Heterocycles, 60, 47-56 (2003).

131. Myoung Goo Kim, Ulrich Strych, Kurt Krause, Michael Benedik, and Harold Kohn,* N(2)-Substituted D,L-Cycloserine Derivatives:  Synthesis and Evaluation as Alanine Racemase Inhibitors, J. Antibiotics, 56, 160-168 (2003).

132. Thomas P. Weber, William R. Widger,* and Harold Kohn,* Metal Dependency for Transcription Factor Rho Activation, Biochemistry, 42, 1652-1659 (2003).

133. Yi Xu, Jerry Johnson, Harold Kohn, and William R. Widger,* ATP Binding to Rho Transcription Termination Factor:  Mutant F355W ATP-induced Fluorescence Quenching Reveals Dynamic ATP Binding, J. Biol. Chem., 278, 13719-13727 (2003).

134. Myoung Goo Kim, Erik T. Bodor, Chen Wang, T. Kendall Harden,* and Harold Kohn,* C(8) Substituted 1-Azabicyclo[3.3.1]non-3-enes and C(8) Substituted 1-Azabicyclo[3.3.1]nonan-4-ones:  Novel Muscarinic Receptor Antagonists, J. Med. Chem., 46, 2216-2226 (2003).

135. Andrew P. Brogan, William R. Widger,* and Harold Kohn,* Bicyclomycin Fluorescent Probes:  Synthesis, Biochemical, Biophysical, and Biological Properties, J. Org. Chem., 68, 5575-5587 (2003).

136. Thomas P. Weber, William R. Widger, and Harold Kohn,* Metal–1,4-Dithio-2,3-dihydroxybutane Chelates:  Novel Inhibitors of the Rho Transcription Termination Factor, Biochemistry, 42, 9121-9126 (2003).

137. Cécile Béguin, Shridhar V. Andurkar, Albert Y. Jin, James P. Stables, Donald F. Weaver, and Harold Kohn,* Functionalized Amido Ketones:  New Anticonvulsant Agents, Bioorg. Med. Chem., 11, 4275-4285 (2003).

138. Myoung Goo Kim, Ulrich Strych, Kurt Krause, Michael Benedik, and Harold Kohn,* Evaluation of Amino-Substituted Heterocyclic Derivatives as Alanine Racemase Inhibitors, Med. Chem. Res., 12, 130-138 (2003).

139. Edwin Vedejs,* B.N. Naidu, Artis Klapars, Don L. Warner, Ven-Shun Li, Younghwa Na, and Harold Kohn,* Synthetic Enantiopure Aziridinomitosenes; Preparation, Reactivity, and DNA Alkylation Studies, J. Am. Chem. Soc., 125, 15796-15806 (2003).

140. Sang Hyup Lee and Harold Kohn,* Cyclic Disulfide C(8) Iminoporfiromycin:  Nucleophilic Activation of a Porfiromycin, J. Am. Chem. Soc., 126, 4281-4292 (2004).

141. Cécile Béguin, Arnaud LeTiran, James P. Stables, and Harold Kohn,* N-Substituted Amino Acid N'-Benzylamides:  Synthesis, Anticonvulsant and Metabolic Activities, Bioorg. Med. Chem., 12, 3079-3096 (2004).

142. Myoung Goo Kim, Erik T. Bodor, T. Kendall Harden,* and Harold Kohn,* C(8) Substituted 1-Azabicyclo[3.3.1]non-3-enes: A Novel Scaffold for Muscarinic Receptor Ligands, Bioorg. Med. Chem., 12, 2357-2367 (2004).

143. Min Shen, Cécile Béguin, Alexander Golbraikh, James P. Stables, Harold Kohn* and Alexander Tropsha,* Application of Predicitive QSAR Models to Database Mining:  Rational Discovery of Novel Anticonvulsant Lead Compounds, J. Med. Chem., 47, 2356-2364 (2004).

144. Emmanuel Skordalakes, Andrew P. Brogan, Boon Saeng Park, Harold Kohn, and James M. Berger,* Structural mechanism of inhibition of the Rho transcription termination factor by the antibiotic bicyclomycin, Structure, 13, 99-109 (2005).

145. Sang Hyup Lee and Harold Kohn,* 7-N,7'-N'-(1'',2''-Dithanyl-3'',6''-dimethylenyl)bismitomycin C:  Synthesis and Nucleophilic Activation of a Dimeric Mitomycin, Organic & Biomolecular Chemistry, 3, 471-482 (2005).

146. Andrew P. Brogan, William R. Widger,* Dalila Bensadek, Isabel Riba-Garcia, Simon J. Gaskell* and Harold Kohn,* Development of a Technique to Determine Bicyclomycin-Rho Binding and Stoichiometry by Isothermal Titration Calorimetry and Mass Spectrometry, J. Am. Chem. Soc. 127, 2741-2751 (2005).

147. Sang Hyup Lee, Robert L. Brodnick, Gary L. Glish, and Harold Kohn,* 3,8,11,16-Tetrakis(aminomethyl)-1,2,9,10-tetrathiacyclohexadecane Tetra-trifluoroacetic Acid:  Synthetic Precursor to a Novel Thio-Substituted Diamine, Tetrahedron, 61, 1749-1754 (2005).

148. Andrew P. Brogan, Jacob Verghese, William R. Widger*, and Harold Kohn,* Bismuth-dithiol inhibition of the Escherichia coli rho transcription termination factor, J. Inorg. Biochem., 99, 841-851 (2005).

149. Pierre LeMagueres, Hookang Im, Jerry Ebalunode, Ulrich Strych, Michael Benedik, James Briggs, Harold Kohn and Kurt L. Krause,* The 1.9 A crystal structure of alanine racemase from Mycobacterium tuberculosis contains a conserved passageway into the active sites, Biochemistry, 44, 1471-1481 (2005).

150. Harold Kohn* and William Widger*, The Molecular Basis for the Mode of Action of Bicyclomycin, Current Drug Targets, in press.

151. Albert Y. Jin, Harold Kohn, Cécile Béguin, Shridhar V. Andurkar, James P. Stables, and Donald F. Weaver,* A Quantitative Structure-Activity Relationship Study for α-Substituted Acetamido-N-Benzylacetamide Derivatives:  A Novel Anticonvulsant Drug Class, Can. J. Chem., 83, 37-45 (2005).