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Secosteroid thiosemicarbazides and secosteroid–1,2,4-triazoles as antiproliferative agents targeting breast cancer cells: Synthesis and biological evaluation Научная публикация

Журнал The Journal of Steroid Biochemistry and Molecular Biology
ISSN: 1879-1220 , E-ISSN: 0960-0760
Вых. Данные Год: 2023, Том: 234, Номер статьи : 106386, Страниц : DOI: 10.1016/j.jsbmb.2023.106386
Авторы Ilovaisky Alexey I. 1 , Scherbakov Alexander M. 2 , Chernoburova Elena I. 1 , Povarov Andrey A. 1 , Shchetinina Marina A. 1 , Merkulova Valentina M. 1 , Salnikova Diana I. 2 , Sorokin Danila V. 2 , Bozhenko Eugene I. 1 , Zavarzin Igor V. 1 , Terent’ev Alexander O. 1
Организации
1 N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, Leninsky prospect 47, Moscow 119991, Russia
2 N.N. Blokhin National Medical Research Center of Oncology, Kashirskoye shosse 24, Moscow 115522, Russia

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
Web of science 2
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