Goel, BharatNaik, AlivaTripathi, NancyKhan, AnjeshBansal, SunilBansal, ShivaniKumar Guru, SantoshJain, Shreyans K.2025-01-282025-01-28202323656549https://dl.bhu.ac.in/ir/handle/123456789/21840In the present work, series of C10-amine and amide derivatives of gloriosine were synthesized and evaluated for in vitro cytotoxic activity against a panel of six human cancer cell lines (MDA-MB-231, U87, FaDu, SiHa, A549, and MCF-7) of multiple tissue origin. The synthesized compounds were characterized by 1H and 13C NMR and MS experiments. In vitro cytotoxicity study showed that most of the C10-amine derivatives demonstrated superior activity in two of the tested cell lines, namely U87 and FaDu cell lines, while C10-amide derivatives showed poor activity in all the cell lines. The C10-amine derivatives were subjected to molecular docking studies to explore their possible binding interactions with colchicine binding site of tubulin protein, and in-silico ADME profiling to study the drug-likeness. The C10-amine derivatives may be less toxic than gloriosine towards normal cells and may provide the lead for anticancer drug development. � 2023 Wiley-VCH GmbH.enAnticancer activityColchicine binding siteGloriosineNatural productsSemi-synthesisTubulinArticlehttps://doi.org/10.1002/slct.202301063