Synthesis of 7-triazole-substituted camptothecin via click chemistry and evaluation of in vitro antitumor activity

Camptothecin (CPT) is a natural topoisomerase I inhibitor with powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers. To discover more potent antitumor agents, a series of new CPT derivatives were synthesized utilizing click chemistry. All compounds were assessed for cytotoxicity against A549, HCT-116, HT-29, LoVo, MDA-MB-231 cell lines, and some compounds exhibited good in vitro potency. Furthermore, all compounds kept or enhanced Topo I inhibition. A series of novel 7-triazole substituted camptothecin via click chemistry was designed, synthesized, and evaluated for their in vitro antitumor activity.