Cytostatic Activity of Combretastatin A-4 Derivatives in an In Vitro System | Sciact

Cytostatic Activity of Combretastatin A-4 Derivatives in an In Vitro System Научная публикация

Журнал

Bulletin of Experimental Biology and Medicine
ISSN: 0007-4888 , E-ISSN: 1573-8221

Вых. Данные

Год: 2022, Том: 174, Номер: 2, Страницы: 221-225 Страниц : 5 DOI: 10.1007/s10517-023-05677-6

Авторы

Plyutinskaya A D ¹ , Nemtsova E R ¹ , Pankratov A A ¹ , Shegai P V ¹ , Krylov S S ² , Iskandarova V N ³ , Maksimenko A S ² , Demchuk D V ² , Kuptsova T S ² , Semenova M N ⁴ , Semenov V V ²

Организации

1	National Medical Research Center of Radiology, Ministry of Health of the Russian Federation, Moscow, Russia
2	N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, Moscow, Russia
3	LLC “Skandiya”, Moscow, Russia
4	N. K. Koltsov Institute of Developmental Biology, Russian Academy of Sciences, Moscow, Russia

Cytostatic activity of combretastatin A-4, its 11 analogues, and paclitaxel (Taxacad) was evaluated in vitro on human tumor cells A549 (lung adenocarcinoma) and PC-3 (prostate adenocarcinoma) in order to find the active and stable compound as a promising antitumor agent. 5-(4-Methoxyphenyl)-4-(3,4,5-trimethoxyphenyl)-isoxazole (compound 123124) and 3-(3,4,5-trimethoxyphenyl)-4-(4-methoxyphenyl)-isoxazole (compound 29310186) demonstrated the highest cytostatic activity (IC50≈8×10—9 М). The activity of two other cytotoxic compounds (2E)-1-(7-methoxy-2H-1,3-benzodioxol-5-yl)-3-(4-methoxyphenyl)prop-2-en-1-one (compound 104815) and 4-(3-amino-4-methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-pyrazole hydrochloride (compound 198732) was close to that of Taxacad: IC50 65×10—9 and 80×10—9 М, respectively, and are also promising active components for the development of antitumor drugs.

Plyutinskaya A.D. , Nemtsova E.R. , Pankratov A.A. , Shegai P.V. , Krylov S.S. , Iskandarova V.N. , Maksimenko A.S. , Demchuk D.V. , Kuptsova T.S. , Semenova M.N. , Semenov V.V.
Cytostatic Activity of Combretastatin A-4 Derivatives in an In Vitro System
Bulletin of Experimental Biology and Medicine. 2022. V.174. N2. P.221-225. DOI: 10.1007/s10517-023-05677-6 WOS Scopus OpenAlex

Web of science:	WOS:000907796300010
Scopus:	2-s2.0-85145593573
OpenAlex:	W4313544963

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