Shchekotikhin, Andrey E.

Graduated from Mendeleev University of Chemical Technology (Master of Science, chemistry) in 1993 where later worked as a postgraduate studies at the Department of Organic chemistry. In 1998 he defended PhD thesis (advisor, Prof. N.N. Suvorov). Since 1996 he worked at the Department of Organic Chemistry at Mendeleev University of Chemical Technology as Head of Laboratory, Assistant (since 2001), Assistant Professor (since 2002) and Professor (since 2010). In 2013 he was promoted to the tenure of the Head of Organic Chemistry Department at Mendeleev University which he holds until now.

In 2001 Dr. Shchekotikhin was hired to Gauze Institute of New Antibiotics (GINA) for the Senior Researcher position at the Laboratory of Chemical Transformation of Antibiotics (Head, Prof. M.N. Preobrazhenskaya). In 2009 he defended Dr. Sci. dissertation "Synthesis, chemical properties and biological activity of heterocyclic analogs of 5,12-naphthacenequinone" (advisor, Prof. M.N. Preobrazhenskaya) and became Doctor of Chemical Sciences in organic chemistry. Since 2010 he worked as a Leading Researcher; in 2015-2017 he combined the positions of GINA Deputy Director and Head of Laboratory of Chemical Transformation of Antibiotics. In 2017 Professor RAS A. Shchekotikhin has been appointed as Director of GINA.

Research interests: Design and synthesis of biologically active heterocyclic compounds and semi-synthetic antibiotics; structure-activity studies; development and preclinical evaluation of chemotherapeutic drugs.

Major publications:

1. Cogoi S., Shchekotikhin A.E., Xodo L.E. HRAS is silenced by two neighboring G-quadruplexesand activated by MAZ, a zinc-finger transcription factor with DNA unfolding property. Nucleic Acids Research. – 2014. – Vol. 42 (13). – p. 8379–8388.
2. Shchekotikhin A.E., Glazunova V.A., Dezhenkova L.G., Luzikov Y.N., Buyanov V.N., Treshalina H.M., Lesnaya N.A., Romanenko V.I., Kaluzhny D.N., Balzarini J., Agama K., Pommier Y., Shtil A.A., Preobrazhenskaya M.N. Synthesis and evaluation of new antitumor 3-aminomethyl-4,11-dihydroxynaphtho[2,3-f]indole-5,10-diones. European Journal of Medicinal Chemistry. – 2014. – Vol. 86. – p. 797-805.
3. Ilyinsky N.S., Shchyolkina A.K., Borisova O.F., Mamaeva O.K., Zvereva M.I., Azhibek D.M., Livshits M.A., Mitkevich V.A., Balzarini J., Sinkevich Y.B., Luzikov Y.N., Dezhenkova L.G., Kolotova E.S., Shtil A.A., Shchekotikhin A.E., Kaluzhny D.N. Novel multi-targeting anthra[2,3-b]thiophene-5,10-diones with guanidine-containing side chains: interaction with telomeric G-quadruplex, inhibition of telomerase and topoisomerase I and cytotoxic properties. European Journal of Medicinal Chemistry. – 2014. – Vol. 85. – p. 605-614.
4. Tikhomirov A. S., Shchekotikhin A. E., Preobrazhenskaya M. N. Methods for the Synthesis and Modification of Linear Anthrafurandiones (Review). Chemistry of Heterocyclic Compounds. – 2014. – Vol. 50 (2). – p 193-208.
5. Tikhomirov A.S. Shchekotikhin A. E., Luzikov Yu.N., Korolev A.M., Preobrazhenskaya M. N. Pd-catalyzed cross-coupling/heterocyclization domino reaction: facile access to anthra[2,3-b]furan-5,10-dione scaffold. Tetrahedron. – 2014. – Vol. 70. – p. 8062-8066.
6. Cogoi S., Shchekotikhin A.E., Membrino A.,Sinkevich Y.B., Xodo L.E. Guanidino anthrathiophenediones as G–quadruplex binders: uptake, intracellular localization and anti Harvey–ras gene activity in bladder cancer cells. Journal Medicinal Chemistry. – 2013. – Vol. 56 (7). – p. 2764–2778.
7. Щекотихин А.Е. Гетероциклические аналоги 5,12–нафтаценхинона. Синтез, свойства, биологическая активность (Монография). LAP Lambert Academic Publishing GmbH. - Saarbrucken, Germany . - 2011. - 500 c.
8. Kaluzhny D., Shchekotikhin A.E., Ilyinsky N., Shchekotikhin A., Sinkevich Y., Tsvetkov P., Tsvetkov V., Veselovsky A., Livshits M., Borisova O., Shtil A., Shchyolkina A. Disordering of human telomeric G–quadruplex with novel antiproliferative anthrathiophenedione. PLoS ONE. – 2011. – vol.6. – №11. – e27151.
9. Shchekotikhin A.E., Glazunova V.A., Dezhenkova L.G., Shevtsova E.K., Traven V.F., Balzarini J., Huang H.S., Shtil A.A., Preobrazhenskaya M.N. The first series of 4,11–bis[(2–aminoethyl)amino]anthra[2,3–b]furan–5,10–diones: Synthesis and anti–proliferative characteristics. Europian Journal of Medicinal Chemistry. – 2011. – Vol. 46. – p.423–428.
10. Shchekotikhin A.E., Glazunova V.A., Dezhenkova L.G., Luzikov Y.N., Sinkevich Y.B., Kovalenko L.V., Buyanov V.N., Balzarini J., Huang F.–C., Lin J.–J., Huang H.–S., Shtil A.A., Preobrazhenskaya M.N Synthesis and cytotoxic properties of 4,11–bis[(aminoethyl)amino]anthra[2,3–b]thiophene–5,10–diones, novel analogues of antitumor anthracene–9,10–diones. Bioorganic and Medicinal Chemistry – 2009. – Vol. 17.– p.1861–1869.
11. Shchekotikhin A.E., Dezhenkova L.G., Susova O.Y., Glazunova V.A., Luzikov Y.N., Sinkevich Y. B., Buyanov V.N., Shtil A.A., Preobrazhenskaya M.N. Naphthoindole–based analogues of tryptophan and tryptamine: synthesis and cytotoxic properties. Bioorganic and Medicinal Chemistry. – 2007 – Vol. 15.– P. 2651–2659.
12. Shchekotikhin A.E., Shtil A.A., Luzikov Y.N., Bobrysheva T.V., Buyanov V.N., Preobrazhenskaya M.N. 3–Aminomethyl derivatives of 4,11–dihydroxynaphtho[2,3–f]indole–5,10–dione for circumvention of anticancer drug resistance. Bioorganic and Medicinal Chemistry.– 2005 – Vol. 13.– №6 – P. 2285 – 2291.
13. Korolev A.M., Shchekotikhin A.E., Lysenkova L.N., Preobrazhenskaya M.N. Synthesis of (indol–3–yl)methansulfoneamide and its 5–methoxy derivative. Synthesis.–2003– № 3.–P. 383 – 388.
14. Pearlstein R.A., Vaz R.J., Kang J., Chen X.–L., Preobrazhenskaya M.N., Korolev A.M., Lysenkova L.N., Miroshnikova O.V., Hendrix J., Rampe D.Characterization of HERG potassium channel inhibition using CoMSiA 3D QSAR and Homology Modeling approaches. Bioorganic and Medicinal Chemistry Letters. –2003 – № 13. – P. 1829 – 1835.
15. Щекотихин А.Е., Баберкина Е.П., Буянов В.Н., Турчин К.Ф., Авраменко Г.В., Суворов Н.Н. Нафтоиндолы.7. Синтез 4,11–диметоксинафто[2,3–f]индол–5,10–диона и 4–метоксинафто[2,3–f]индол–5,10–диона. Химия Гетероциклических Соединений. – 1996. – № 8.–С.1050 – 1054.

ПАТЕНТЫ:

1. Щекотихин А.Е., Тихомиров А.С., Ильинский Н.С., Калюжный Д.Н., Щелкина А.К., Борисова О.Ф., Лившиц М.А., Цветков В.Б., Бычкова Е.Н., Малютина Н.М., Деженкова Л.Г., Штиль А.А., Преображенская М.Н. Новые лиганды G-квадруплексов на основе гетероаренантрацендионов, ингибирующие рост опухолевых клеток. Патент РФ № 2527459 (2014).
2. Щекотихин А.Е., Тихомиров А.С., Синькевич Ю.Б., Деженкова Л.Г., Ксодо Л., Резникова М.И., Трещалина Е.М., Штиль А.А., Преображенская М.Н. Мультитаргетные ингибиторы опухолевого роста на основе линейных гетероаренантрацендионов. Патент РФ № 2527273 (2014).
3. Лашков А.А., Щекотихин А.Е., Сотниченко С.Е., Штиль А.А., Михайлов А.М. Ингибитор уридинфосфорилаз. Патент РФ № 2522548 (2014).
4. Щекотихин А.Е., Преображенская М.Н., Синькевич Ю.Б., Штиль А.А., Глазунова В.А., Трещалин И.Д., Трещалина Е.М. Цитотоксические линейные гетероциклические производные антрацендиона, содержащие в боковой цепи циклические диамины, активные в отношении опухолевых клеток с Множественной Лекарственной Устойчивостью. Патент РФ № 2412166 (2011).