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SYNTHESIS VIA THE MANNICH REACTION AND BIOLOGICAL ACTIVITY OF NOVEL FLUORINATED CAMPTOTHECIN DERIVATIVES

Chuanhao Wang, Yuan Wang, Haijun Ma, Yazhao Zhu, Yanming Zhang, Zhenyuan Miao, Yuelin Wu
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Abstract


Two series of fluorinated camptothecin derivatives had been designed and synthesized via the Mannich reaction. The hexacyclic fluorinated camptothecin derivatives were found to be more active. (9S,10S)-2-Cyclopropyl-9-ethyl-10-fluoro-9-hydroxy-2,3,9,10,12,15-hexahydro-1H,13H-[1,3]oxazino[5,6-f]pyrano[3',4':6,7]indolizino[1,2-b]quinolin-13-one showed potent antitumor activity against A549 and T24 cell lines with effective topoisomerase I inhibitory activity.


Keywords


fluorinated camptothecin; antitumor activity; Mannich reaction; natural products.

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