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Secosteroid–quinoline hybrids as new anticancer agentsстатья Исследовательская статья
- Авторы: Ilovaisky Alexey I., Scherbakov Alexander M., Merkulova Valentina M., Chernoburova Elena I., Shchetinina Marina A., Andreeva Olga E., Salnikova Diana I., Zavarzin Igor V., Terent’ev Alexander O.
- Журнал: Journal of Steroid Biochemistry and Molecular Biology
- Год издания: 2023
- Издательство: Pergamon Press Ltd.
- Местоположение издательства: United Kingdom
- Номер статьи: 106245
- DOI: 10.1016/j.jsbmb.2022.106245
- Аннотация: 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 secosteroids 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’-quinolylmethylene]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.
- Добавил в систему: Сальникова Диана Игоревна