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Преподаватели и сотрудники

Щекотихин Андрей Егорович

Щекотихин Андрей Егорович

Должность Заведующий кафедрой
Телефон (499) 978-94-01
E-mail shchekotikhin@muctr.ru
Сайт https://muctr.ru
Уровень образования Высшее
Преподаваемые дисциплины

Органическая химия (1.2)

Химические основы биологических процессов

Методы современного органического синтеза

Практикум по органической химии

Учёная степень Доктор химических наук
Учёное звание Доцент
Наименование направления подготовки и (или) специальности Инженер химик-технолог по специальности «Ядерная химическая технология»
Данные о повышении квалификации и (или) профессиональной переподготовке

«Аккредитация вуза в условиях ФГОС++», ФГБОУ ВО РХТУ им. Д.И. Менделеева, 18 часов, повышение квалификации, с 5.02.2018 по 19.03.2018 г., 771801452835 от 19.03.2018

«Противодействие коррупции», ФГБОУ ВО РХТУ им. Д.И. Менделеева, 40 часов, повышение квалификации, 772402001988 от 16.10.2015

Общий стаж работы 22 года (с 01.11.1996)
Стаж работы по специальности 19 лет (с 01.09.1999)

Публикации

Atp-synthase inhibition by semi-synthetic oligomycin a derivatives / O. A. Omelchuk, D. A. Mavletova, T. A. Koshenko et al. // FEBS open bio. — 2018. — Vol. 8, no. S1. — P. 487–487. [ DOI ]

Tikhomirov A. S., Shtil A. A., Shchekotikhin A. E. Advances in the discovery of anthraquinone-based anticancer agents // Recent Patents on Anti-Cancer Drug Discovery. — 2018. — Vol. 13, no. 2. Background: The anthracene-9,10-dione (anthraquinone) derivatives represent an exceptionally valuable class in anticancer drug development. An outstanding antitumor potency of the anthracycline antibiotics attracted the attention of medicinal chemists since the discovery of these chemotypes. The prominent anthraquinone-based drugs doxorubicin, mitoxantrone as well as more recent epirubicin, idarubicin, and valrubicin are successfully used in chemotherapy of hematological malignancies and solid tumors. The anthraquinone core remains a promising scaffold for the search of new optimized drug candidates. Objective: In this study, we analyze the progress in discovery and development of antitumor anthracene- 9,10-diones based on patent and journal publications in 2008-2017. The main goal is to dissect novel chemotypes of anthraquinone derivatives; other important issues such as the success in bioconjugate chemistry of anthraquinone containing agents as well as the patents on new applications of anthracyclines are beyond the scope of this review. Conclusion: A number of newly discovered natural products, the perspective directions for chemical modifications to optimize the anticancer properties, and novel intracellular targets demonstrate that anthracene- 9,10-diones deserve further in-depth investigation as an important source of drug candidates. [ DOI ]

Aminomethylation of heliomycin: Preparation and anticancer characterization of the first series of semi-synthetic derivatives / G. Y. Nadysev, A. S. Tikhomirov, M.-H. Lin et al. // European Journal of Medicinal Chemistry. — 2018. — Vol. 143. — P. 1553–1562. Abstract A series of 4-aminomethyl derivatives of heliomycin 1 was prepared using the Mannich reaction. The modification significantly improved aqueous solubility of the initially poorly soluble antibiotic. Testing the antiproliferative efficacy revealed a potent activity of heliomycin as well as its new derivatives on a panel of mammalian tumor cells including drug resistant variants. In contrast to 1 the new derivatives 7a, 7l, 7p generated a high level of ROS associated with induction of apoptosis in T24 bladder cancer cells. Introduction of 4-aminomethyl moiety increased the affinity to DNA and the ability to inhibit topoisomerase 1 making 7p the most promising candidate for further preclinical evaluation. Thus, aminomethylation is the first-in-class successful transformation of the antibiotic 1 resulting in an improved water solubility of derivatives and promising properties in search of novel anticancer drug candidates. [ DOI ]

Heterocyclic analogs of 5,12-naphthacenequinone 15*. synthesis of new anthra[2,3-b]thiophene-3(2)-carboxylic acids / D. V. Andreeva, Y. B. Sinkevich, A. S. Tikhomirov et al. // Chemistry of Heterocyclic Compounds. — 2018. — Vol. 54, no. 6. — P. 612–617. [ DOI ]

New antitumor anthra[2,3-b]furan-3-carboxamides: Synthesis and structure-activity relationship / A. S. Tikhomirov, L. Chia-Yang, Y. L. Volodina et al. // European Journal of Medicinal Chemistry. — 2018. — Vol. 148. — P. 128–139. Chemical modifications of the anthraquinone scaffold are aimed at optimization of this exceptionally productive class of antitumor drugs. In particular, our previously reported anthra[2,3-b]furan-3- carboxamides demonstrated a high cytotoxic potency in cell culture and in vivo. In this study, we expanded our series of anthra[2,3-b]furan-3-carboxamides by modifying the key functional groups and dissected the structure-activity relationship within this chemotype. The majority of new compounds inhibited the growth of mammalian tumor cell lines at submicromolar to low micromolar concentrations. We found that 4,11-hydroxy groups as well as the carbonyl moiety in the carboxamide fragment were critical for cytotoxicity whereas the substituent at the 2-position of anthra[2,3-b]furan was not. Importantly, the new derivatives were similarly potent against wild type cells and their variants resistant to doxorubicin due to P-glycoprotein (Pgp) expression or p53 inactivation. The most cytotoxic derivatives 6 and 9 attenuated plasmid DNA relaxation by topoisomerase 1. Finally, we demonstrated that 6 and 9 at 1 mM induced intracellular oxidative stress, accumulation in G2/M phase of the cell cycle, and apoptosis in gastric carcinoma cell lines regardless of their p53 status. These results further substantiate the potential of anthra[2,3-b]furan-3-carboxamides as antitumor drug candidates. [ DOI ]

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