Abstract: An elegant approach to unknown secosteroid–quinoline hybrids is disclosed. A series of 13,17-secoestra-1,3,5(10)-trien-17-oic acid [N′ -(iso)quinolylmethylene]hydrazides was prepared and these novel type of secoste-roids was screened for antiproliferative activity against estrogen-responsive human breast cancer cell line MCF-7. Most of the synthesized compounds showed a cytotoxic effect superior to that of reference drug cisplatin; the lead compound exhibits the highest activity with the IC50 value of about 0.8 μM and is 7 times more active than cisplatin. A high selectivity index was observed for the hit 13,17-secoestra-1,3,5(10)-trien-17-oic acid [N′ -qui-nolylmethylene]hydrazides 2a and 2c. Compounds 2a and 2c evaluated in luciferase reporter assays exhibited high antiestrogenic potency which was superior to that of tamoxifen. These hit compounds were characterized by high activity against MCF-7 cells that retained towards multidrug-resistant NCI/ADR-RES cells.

Cite: Ilovaisky A.I. , Scherbakov A.M. , Merkulova V.M. , Chernoburova E.I. , Shchetinina M.A. , Andreeva O.E. , Salnikova D.I. , Zavarzin I.V. , Terent’ev A.O.
Secosteroid–quinoline hybrids as new anticancer agents
The Journal of Steroid Biochemistry and Molecular Biology. 2023. V.228. 106245 :1-13. DOI: 10.1016/j.jsbmb.2022.106245 WOS Scopus OpenAlex

Identifiers:

Web of science:	WOS:000923659100001
Scopus:	2-s2.0-85146153604
OpenAlex:	W4313530105

Citing:

DB	Citing
OpenAlex	10
Web of science	4
Scopus	6

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