Synthesis and evaluation of novel marine bromopyrrole alkaloid-based hybrids as anticancer agents

• A series of 23 novel hybrids of marine bromopyrrole alkaloids were synthesized.
• Hybrids contain chalcone, isoxazole and flavone structural features.
• Hybrids were evaluated for in vitro anticancer activity by MTT assay.
• Thirteen exhibited promising anticancer activity.

A series of twenty three novel hybrids of marine bromopyrrole alkaloids with chalcone, isoxazole and flavone structural features were synthesized and evaluated for in vitro anticancer activity by MTT assay against five human cancer cell lines. Among the synthesized chalcones, hybrids 4a and 4h (IC50 range: 0.18 μM–12.00 μM) showed anticancer activity against all the tested cancer cell lines. Promising cytotoxic activities were exhibited by flavones derivatives, 5a and 5b (0.41 μM–1.28 μM) against cell lines PA1 and KB403. Isoxazole hybrids, 6b–6e selectively inhibited oral and mouth cancer cell line KB403, among which 6c (IC50 = 2.45 μM) was found to be most active.

A series of twenty three novel hybrids of marine bromopyrrole alkaloids with chalcone, isoxazole and flavone structural features were synthesized and evaluated for in vitro anticancer activity by MTT assay.Figure optionsDownload as PowerPoint slide