Syntheses and biological activity of C-3′-difluoromethyl-taxoids
Syntheses and biological activity of C-3′-difluoromethyl-taxoids
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DOI：
10.1016/s0968-0896(00)00093-6
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发表时间：
2000-07-01
影响因子：
3.5
通讯作者：
Scambia, G
中科院分区：
文献类型：
--
作者：
Ojima, I;Lin, SN;Scambia, G
合成了一系列C-3'位含二氟甲基、C-10和C-14位经修饰的紫杉烷类化合物，并对其生物活性进行了研究。体外细胞毒性试验结果表明，与紫杉醇相比，这些新开发的紫杉烷类化合物对药物敏感细胞系LCC 6-WT的活性提高了几倍，对相应的耐药癌细胞系LCC 6-MDR的活性提高了40-70倍。细胞凋亡分析揭示了SB-T-12843（Ie）在携带MDR和MDR阴性癌细胞中诱导细胞凋亡的异常活性。(C)2000爱思唯尔科技有限公司版权所有。
A series of new taxoids bearing difluoromethyl group at the C-3' position and modifications at the C-10 and C-14 positions has been synthesized and their biological activities studied. The in vitro cytotoxicity assay results indicate that these newly developed taxoids exhibit comparable to several times better activity against drug-sensitive cell line LCC6-WT, and 40-70 times better activity against the corresponding drug-resistant cancer cell line LCC6-MDR as compared to that of paclitaxel. Apoptosis analysis has revealed the exceptional activity of SB-T-12843 (le) in inducing apoptosis in both MDR-bearing and MDR-negative cancer cells. (C) 2000 Elsevier Science Ltd. All rights reserved.