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.

中文翻译：

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新型氟化喜树碱衍生物的曼尼希反应合成及生物活性

通过曼尼希反应设计并合成了两个系列的氟化喜树碱衍生物。发现六环氟化喜树碱衍生物更具活性。(9 S ,10 S )-2-Cyclopropyl-9-ethyl-10-fluoro-9-hydroxy-2,3,9,10,12,15-hexahydro-1 H ,13 H -[1,3]oxazino [5,6- f ]pyrano[3',4':6,7]indolizino[1,2 - b ]quinolin-13-one 对 A549 和 T24 细胞系具有有效的抗肿瘤活性，具有有效的拓扑异构酶 I 抑制活性。