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Synthesis of 7‐Triazole‐substituted Camptothecin via Click Chemistry and Evaluation of in vitro Antitumor Activity
Author(s) -
Wang Lei,
Yuan Wei,
Zhang Jie,
Tong Linjiang,
Luo Yu,
Chen Yi,
Lu Wei,
Huang Qingqing
Publication year - 2014
Publication title -
chinese journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.28
H-Index - 41
eISSN - 1614-7065
pISSN - 1001-604X
DOI - 10.1002/cjoc.201300703
Subject(s) - chemistry , camptothecin , in vitro , click chemistry , cytotoxicity , potency , topoisomerase , triazole , pharmacology , combinatorial chemistry , stereochemistry , biochemistry , organic chemistry , medicine
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.