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Updated: Dec 15, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Fe(iii)-Catalyzed synthesis of steroidal imidazoheterocycles as potent antiproliferative agents
Sadhanendu Samanta1, Asim Kumar Ghosh, Sumit Ghosh
1Department of Chemistry, Visva-Bharati (A Central University), Santiniketan, 731235, West Bengal, India. alakananda.hajra@visva-bharati.ac.in.
Abstract:
An efficient and practical method has been developed for the synthesis of steroidal imidazoheterocycles via cost-effective and environmentally benign FeCl3-catalyzed oxidative amination. A library of steroidal imidazo[1,2-a]pyridines was directly synthesized from readily available 2-aminopyridines and steroidal ketones in aerobic conditions. The synthesized compounds were screened for activity on human microsomal cytochrome P450s CYP7, CYP17 and CYP21. Antiproliferative activity of two lead compounds 3ia and 3la was additionally evaluated against the human MCF-7 (breast cancer), SKOV3 (ovarian cancer), and 22Rv1 (prostate cancer) cell lines. Steroidal imidazo[1,2-a]pyridine 3la which is a substrate molecule for CYP17A1 with IC50 = 1.7 μM (MCF-7), 3.0 (SKOV3), and 6.0 μM (22Rv1) has proved to be more active than reference drug cisplatin.
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