Secosteroidal hydrazides: Promising scaffolds for anti-breast cancer agents

Secosteroidal hydrazides: Promising scaffolds for anti-breast cancer agents Full article

Journal

The Journal of Steroid Biochemistry and Molecular Biology
ISSN: 1879-1220 , E-ISSN: 0960-0760

Output data

Year: 2021, Volume: 214, Article number : 106000, Pages count : DOI: 10.1016/j.jsbmb.2021.106000

Authors

Ilovaisky Alexey I. ¹ , Merkulova Valentina M. ¹ , Chernoburova Elena I. ¹ , Shchetinina Marina A. ¹ , Salnikova Diana I. ² , Scherbakov Alexander M. ² , Zavarzin Igor V. ¹ , Terent’ev Alexander O. ¹

Affiliations

1	N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, 47 Leninsky prosp., 119991, Moscow, Russia
2	Department of Experimental Tumor Biology, N.N. Blokhin National Medical Research Center of Oncology of the Ministry of Health of the Russian Federation, 24 Kashirskoye sh., Moscow, 115522, Russia

A convenient and selective approach to 13,17-secoestra-1,3,5(10)-trien-17-oic acid hydrazides and their N’-(het)arylmethylene derivatives was disclosed and these novel types of secosteroids were screened for cytotoxicity against hormone-dependent human breast cancer cell line MCF-7. A number of 13,17-secoestra-1,3,5(10)-trien-17-oic acid [N’-(het)arylmethylene]hydrazides show significant cytotoxic effect comparable or superior to that for reference drug cisplatin. Compound 3l exhibits the highest activity with the IC50 value of about 2 μM and is 2.8 times more active than cisplatin. Hit 13,17-secoestra-1,3,5(10)-trien-17-oic acid [N’-(het)arylmethylene]hydrazides 3d, 3l and 3q are characterized by high cytotoxicity and good selectivity towards MCF-7 breast cancer cells. The synthesized secosteroids may be considered as new promising antitumor agents.

Ilovaisky A.I. , Merkulova V.M. , Chernoburova E.I. , Shchetinina M.A. , Salnikova D.I. , Scherbakov A.M. , Zavarzin I.V. , Terent’ev A.O.
Secosteroidal hydrazides: Promising scaffolds for anti-breast cancer agents
The Journal of Steroid Biochemistry and Molecular Biology. 2021. V.214. 106000 . DOI: 10.1016/j.jsbmb.2021.106000 WOS Scopus OpenAlex

Web of science:	WOS:000701839300003
Scopus:	2-s2.0-85115365104
OpenAlex:	W3201600383

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OpenAlex	8
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