Synthesis of 7‐Triazole‐substituted Camptothecin via Click Chemistry and Evaluation of in vitro Antitumor Activity |
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| Authors: | Lei Wang Wei Yuan Jie Zhang Linjiang Tong Yu Luo Yi Chen Wei Lu Qingqing Huang |
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| Institution: | 1. Institute of Drug Discovery and Development, Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, Shanghai 200062, China;2. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, SIBS, Chinese Academy of Sciences, Shanghai 201203, China |
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| 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. |
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| Keywords: | camptothecin 7‐triazole‐substituted camptothecin click chemistry antitumor |
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