Реферат: A convenient and selective approach to 13,17-secoestra-1,3,5(10)-trien-17-oic acid [N’-arylcarbothioamido]hydrazides and hybrid molecules containing secosteroid and 1,2,4-triazole fragments was disclosed and these novel types of secosteroids were screened for cytotoxicity against hormone-dependent human breast cancer cell line MCF-7. Most of secosteroid–1,2,4-triazole hybrids showed significant cytotoxic effect comparable or superior to that of the reference drug cisplatin. Hit secosteroid–1,2,4-triazole hybrids 4b and 4h were characterized by high cytotoxicity and good selectivity towards MCF-7 breast cancer cells. PARP cleavage (marker of apoptosis) and ERα and cyclin D1 downregulation were discovered in MCF-7 cells treated with lead secosteroid–1,2,4-triazole hybrid 4b. The synthesized secosteroids may be considered as new promising anticancer agents.

Библиографическая ссылка: Ilovaisky A.I. , Scherbakov A.M. , Chernoburova E.I. , Povarov A.A. , Shchetinina M.A. , Merkulova V.M. , Salnikova D.I. , Sorokin D.V. , Bozhenko E.I. , Zavarzin I.V. , Terent’ev A.O.
Secosteroid thiosemicarbazides and secosteroid–1,2,4-triazoles as antiproliferative agents targeting breast cancer cells: Synthesis and biological evaluation
The Journal of Steroid Biochemistry and Molecular Biology. 2023. V.234. 106386 . DOI: 10.1016/j.jsbmb.2023.106386 WOS Scopus OpenAlex

Идентификаторы БД:

Web of science:	WOS:001073885100001
Scopus:	2-s2.0-85175316674
OpenAlex:	W4386390432

Цитирование в БД:

БД	Цитирований
OpenAlex	2
Scopus	2

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