Synthesis of 7‐Triazole‐substituted Camptothecin via Click Chemistry and Evaluation of in vitro Antitumor Activity

Abstract

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.

Postsynthetic Modification of Metal‐Organic Frameworks through Click Chemistry

“…Postsynthetic modification (PSM), [30][31][32][33][34] as an alternative and simple method, has been widely used to functionalize MOFs in recent years. [36][37][38][39][40][41] Click chemistry, [42][43][44] which can proceed the reaction efficiently with high yields and high specificity in the presence of various functional groups, has received a great deal of use in different fields, for example, dendrimer synthesis [45,46] and surface science. Therefore, isoreticular MOFs with the same network topology can be prepared, and the resulting MOFs may show enhanced properties for specialized applications.…”

Molecular Hybridization of Alkaloids Using 1,2,3-Triazole-Based Click Chemistry

“…Three products with R = n-Bu, Bn, and −(CH 2 ) 4 COOMe showed excellent in vitro activity. Moreover, all of the products 3 maintained their inhibitory ability against Topoisomerase I [57].…”

Alkaloids and Isoprenoids Modification by Copper(I)-Catalyzed Huisgen 1,3-Dipolar Cycloaddition (Click Chemistry): Toward New Functions and Molecular Architectures

“…Three of them, with R = Bu, Bn, and −(CH 2 ) 4 COOMe showed in vitro very good activity and all of the products 63 retained the inhibitory potency toward Topo I. 83…”

“…After deprotection of camptothecin ester final products 63 were assessed for their cytotoxicity against A549, HCT-116, HT-29, LoVo, and MDA-MB-231 cell lines. Three of them, with R = Bu, Bn, and −(CH 2 ) 4 COOMe showed in vitro very good activity and all of the products 63 retained the inhibitory potency toward Topo I …”