紫杉醇（泰素）的N-（芳基硫烷基）羰基类似物的合成及生物学评价
Synthesis and biological evaluation of N-(arylsulfanyl)carbonyl analogues of paclitaxel (taxol).
作者信息
Karliga Bekir, Schilling Jennifer K, Kingston David G I, Bane Susan, Ravindra Rudy, Talinli Naciye
机构信息
Istanbul Technical University, Faculty of Science and Letters, Chemistry Department, Maslak, TR-34469, Istanbul, Turkey.
出版信息
Chem Biodivers. 2006 Apr;3(4):396-404. doi: 10.1002/cbdv.200690043.
Four new N-(arylsufanyl)carbonyl paclitaxel analogues (2a-d) were prepared from 7-(triethylsilyl)-protected baccatin III (5). Their cytotoxicities against human ovarian (A2780) and prostate cancer (PC3) cell lines, as well as their tubulin-assembly activities, were determined. In these assays, the new compounds showed rather weak activities, one two orders of magnitude below those of paclitaxel (taxol; 1). The known 3'-N-[(thiophen-2-yl)carbonyl] paclitaxel analogue 3 was also prepared. As previously reported, 3 exhibited strongly improved cytotoxicities and tubulin-assembly activities as compared to paclitaxel (1).
从7-(三乙基硅基)保护的浆果赤霉素III（5）制备了四种新型N-(芳基硫烷基)羰基紫杉醇类似物（2a-d）。测定了它们对人卵巢癌（A2780）和前列腺癌（PC3）细胞系的细胞毒性以及它们的微管蛋白组装活性。在这些测定中，新化合物显示出相当弱的活性，比紫杉醇（紫杉醇；1）低两个数量级。还制备了已知的3'-N-[(噻吩-2-基)羰基]紫杉醇类似物3。如先前报道的那样，与紫杉醇（1）相比，3表现出显著提高的细胞毒性和微管蛋白组装活性。
Zotero 插件