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Paper | Regular issue | Vol 100, No. 5, 2020, pp.790-801
Published online, 10th April, 2020
DOI: 10.3987/COM-20-14248
Synthesis and Cytotoxic Evaluation of Steroidal Endoperoxide Derivatives with Hydrazide Side Chain as Anticancer Agents

Yinglong Han, Yu Lin, Yongmei Wang, Haijun Wang, Hongling Li, Jing Wang, Yukun Ma, and Ming Bu*

*College of Pharmacy, Qiqihar Medical University, No 333, Bukui North Street, Jianhua District, Qiqihar, China

Abstract

A series of novel steroidal 5α,8α-endoperoxide derivatives bearing hydrazide side chain were synthesized and evaluated for their cytotoxicities in four human cancer cell lines (HepG2, HCT-116, MCF-7, and A549) using the MTT assay in vitro. The results showed that compound 6k exhibited significant cytotoxic activity against HepG2 cells (IC50 = 5.60 μM). Further cellular mechanism studies in HepG2 cells indicated that compound 6k triggered the mitochondrial-mediated apoptosis by decreasing mitochondrial membrane potential (MMP) which was associated with up-regulation of Bax, down-regulation of Bcl-2.