Publications and Patents

Preparation of Trifluoromethylpyridine Libraries, A. M. Shestopalov, V. P. Kislyi, E. Ya. Kruglova, et al, J. Comb. Chem., 2000, 2(1), 24-28.

Fluorine as an NMR Probe for Structural Studies of Chemical and Biological Systems, Y. G. Gakh, A. A. Gakh, A. M. Gronenborn, Magn. Reson. Chem., 2000, 38, 551-558.

Synthetic utilization of polynitroaromatic compounds. 1. S-derivatization of 1-substituted 2,4,6-trinitrobenzenes with thiols, S. G. Zlotin, P. G. Kislitsin, A. V. Samet, E.A., et al, J. Org. Chem., 2000, 65(25), 8430-8438.

Synthetic utilization of polynitroaromatic compounds. 2. Synthesis of 4,6-dinitro-1,2-benzisothiazol-3-ones and 4,6-dinitro-1,2-benzisothiazoles from 2-benzylthio-4,6-dinitrobenzamides, S. G. Zlotin, P. G. Kislitsin, A. I. Podgursky, et al, J. Org. Chem., 2000, 65(25), 8439-8443.

Modular Chemical Descriptor Language (MCDL): Composition, Connectivity, and Supplementary Modules, A. A. Gakh, M. N. Burnett, J. Chem. Inf. Comput. Sci., 2001, 41 (6), 1494-1499.

An Improved "One Pot" Procedure for Synthesis of Fluorinated DL-Phenylalanines, A. V. Samet, D. J. Coughlin, A. C. Buchanan, et al, Synth. Commun., 2002, 32(6), 941-946.

Synthetic Utilization of Polynitroaromatic Compounds. 4. Synthesis of Nitro-Free 4,6-Disubstituted 3-Aminobenzothiophene Derivatives Based on 2,4,6-Trinitrobenzamide, S. G. Zlotin, P. G. Kislitsin, F. A. Kucherov, et al, Heterocycles, 2006, 68(6), 1109-1119.

Synthetic Utilization of Polynitro Aromatic Compounds. 5. Multi-Centered Reactivity Pattern in Reactions of 4,6-Dinitro-1,2-benzoisothiazoles and -isothiazol-3(2H)-ones with C-, N-, O-, S-, and F-Nucleophiles, S. G. Zlotin, P. G. Kislitsin, F. A. Kucherov, et al, Heterocycles, 2006, 68(12), 2483-2498.

Original Approach to New Derivatives of [1,3]Oxazolo[4,5-d]pyrimidine, V. M. Sviripa, A. A. Gakh, V. S. Brovarets, Synthesis, 2006, 20, 3462-3466.

A Java Chemical Structure Editor Supporting the Modular Chemical Descriptor Language (MCDL), S. V. Trepalin, A. V. Yarkov, I. V. Pletnev, et al, Molecules, 2006, 11, 219-231.

Original Recyclization of S-phenacyl Derivatives of 4-Acylamino-2-mercapto-1,3-oxazoles and Their Analogues, A. G. Balia, A. G. Belyuga, V. S. Brovarets, et al, Heteroatom Chem., 2007, 18(4), 432-437.

A Facile Synthesis of New 1,2-Dihydro-2-λ(5)-[1,3]oxazolo[5,4-d][1,3,2]diazaphosphinine Derivatives Starting from 2-Benzoylamino-3,3-dichloroacrylonitrile, O. V. Shablykin, A. A. Gakh, V. S. Brovarets, et al, Heteroatom Chem., 2008, 19(5), 506-511.

Synthesis of 3-cyano-2-fluoropyridines, A. M. Shestopalov, L. A. Rodinovskaya, A. E. Fedorov, et al, J. Fluor. Chem., 2009, 130(2), 236-240.

Trifluoromethoxy containing azoles and azines: synthesis and biological activity, M. V. Vovk, O. M. Pinchuk, V.A. Sukach, et al, in ACS Symposium Series, 2009, vol. 1003, pp. 307-345.

Cascade Iodination-fluorination Synthesis of 2-Fluorothiophene and 5-Fluoro-2-thienyliodonium salts, P. P. Onys'ko, T. V. Kim, O. I. Kiseleva, et al, J. Fluor. Chem., 2009, 130(5), 501-204.

Synthesis and reactions of fluorinated nicotinonitriles, A. M. Shestopalov, L. A. Rodinovskaya, A. A. Shestopalov, et al, in ACS Symposium Series, 2009, vol. 1003, pp. 263-280.

Discovery and Potency Optimization of 2-Amino-5-arylmethyl-1,3-thiazole Derivatives as Potential Therapeutic Agents for Prostate Cancer, M. Krasavin, R. Karapetian, I. Konstantinov, et al, Archiv Der Pharmazie, 2009, 342(7), 420-427.

Microwave-assisted Synthesis of Substituted Fluoroazines Using KF•2H₂O, A. M. Shestopalov, A. E. Fedorov, L. A. Rodinovskaya, et al, Tetrahedron Lett., 2009, 50(37), 5257-5259.

Discovery and SAR exploration of N-aryl-N-(3-aryl-1,2,4-oxadiazol-5-yl)amines as potential therapeutic agents for prostate cancer, M. Krasavin, K. A. Rufanov, A. V. Sosnov, et al, Chem. Cent. J., 2010, 4, 4.

Synthesis of new heterocyclic system of 4,5,7,8-tetrahydroimidazo[1,2-c][1,3] thiazolo [4,5-e][1,3,2] diazaphosphinine starting from 2-aroylamino-3,3-dichloroacrylonitrile, A.P. Kozachenko, O.V. Shablykin, A. A. Gakh, et al, Heteroatom Chem., 2010, 21(7), 492-498.

Synthesis of 1-(4-trifluoromethoxyphenyl)-2,5-dimethyl-3-(2-R-thiazol-4-yl)-1H-pyrroles via chain heterocyclization, M. V. Vovk, O. M. Pinchuk, A. O. Tolmachov, et al, Molecules, 2010, 15(2), 997-1006.

Synthesis of 3-fluoroimidazo[1,2-a]pyrimidines and 5-fluoroimidazo[2,1-b][1,3]thiazoles via heterocyclization of (N-heteroarylimino)trifluoropyruvate, Y. V. Rassukana, Y. Y. Khomutnyk, P. P. Onys'ko, et al, J. Fluor. Chem, 2010, 131(10), 1044-1048.

Extreme modulation properties of aromatic fluorine, A. A. Gakh, M. N. Burnett, J. Fluor. Chem., 2011, 132(2), 88-93.

Modular Chemical Descriptor Language (MCDL): stereochemical modules, A. A. Gakh, M. N. Burnett, S. V. Trepalin, et al, J. Cheminform., 2011, 3, 5.

Anti-cancer agents based on 6-trifluoromethoxybenzimidazole derivatives and method of making, A. A. Gakh, M. V. Vovk, N. V. Mel'nychenko, et al, U.S. Patent 8,242,284, August 14, 2012.

Anti-cancer agents based on 4-(hetero) ary1-1,2,5-oxadiazol-3-yl amino derivatives and a method of making, A. A. Gakh, M. Krasavin, R. Karapetian, et al, U.S. Patent 8,362,047, January 29, 2013.

Identification of diaryl 5-amino-1,2,4-oxadiazoles as tubulin inhibitors: The special case of 3-(2-fluorophenyl)-5-(4-methoxyphenyl) amino-1,2,4-oxadiazole, A.A. Gakh, A.V. Sosnov, M. Krasavin, et al,. Bioorganic & Medicinal Chemistry Letters, 2013, 23(5), 1262-1268.

Anti-cancer agents based on N-acyl-2,3-dihydro-1H-pyrrolo [2,3-b] quinoline derivatives and a method of making, A.A. Gakh, M. Krasavin, R. Karapetian, et al, U.S. Patent 8,420,815, April 16, 2013.

Trifluoromethylated Heterocycles, A.A. Gakh, Y. Shermolovich, Current Topics in Medicinal Chemistry, 2014, 14(7), 952-965.

Antiproliferative 4-(1,2,4-oxadiazol-5-yl) piperidine-1-carboxamides, a new tubulin inhibitor chemotype, M. Krasavin, A.V. Sosnov, R. Karapetian, et al, Bioorganic & Medicinal Chemistry Letters, 2014, 24(18), 4477-4481.