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Updated: Aug 30, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Design, Synthesis and Anticancer Activity of Novel Steroidal Derivatives with D-Ring Fused or Substituted
Xiao-San Li1,2, Mao-Xun Yang1,3, Yu-Hao Luo1
1Guangdong Provincial Key Laboratory of Research and Development of Natural Drugs, Key Laboratory of Research and Development of New Medical Materials of Guangdong Medical University, School of Pharmacy, Guangdong Medical University, Dongguan, 523808, P. R. China.
Abstract:
A series of novel D-ring fused or substituted steroidal N-heterocycles were synthesized, and their chemical structures were characterized by spectroscopic analysis. The anticancer activity of these compounds against four human cancer cell lines (MCF-7, H1299, HeLa and HepG2) were evaluated and the structure-activity relationship (SAR) was also investigated. Compound 3c displayed significant inhibitory activity on the four cancer cells with IC50 values ranging from 3.88 to 10.05 μM. Overall, these studies indicated that construction of N-heterocyclic system with D-ring substituted containing a double bond at C-16 and C-17 or D-ring fused with [17,16-d]azolo[1,5-a]pyrimidine could be a promising strategy to improve antitumor activity for steroids deserved further investigation.
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