【摘 要】
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Taxoids remain a subject of research for the design of novel anticancer drugs and much more complete knowledge of their interaction with microtubules.1-DeoxybaccatinⅥ 1 possessing the typical tetracyc
【机 构】
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Department of Chemistry,Shanghai University,Shanghai 200444
【出 处】
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第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会
论文部分内容阅读
Taxoids remain a subject of research for the design of novel anticancer drugs and much more complete knowledge of their interaction with microtubules.1-DeoxybaccatinⅥ 1 possessing the typical tetracyclic taxoid core while lacking the C-1 hydroxy group is readily available.Herein,taxanes 12 and 13 were successfully synthesized from 1-deoxybaccatinⅥ(Scheme 1).We have also obtained the X-ray structure of taxane 12.1-Deoxytaxane analog 13 showed five-fold improved activity than paclitaxel,while analog 12 exhibited six-fold decreased cytotoxic activities than paclitaxel against the A 549(human lung carcinoma) and MCF-7(human breast carcinoma) cell lines.These amazing results were in good agreement with our previous assumption that the substituent at C-4 was involved in the intimate tubulin binding;therefore,modification of C-4 hydroxyl group holds great promise for discovery of new analogs with enhanced properties.All the compounds were confirmed by 1H-NMR,13C-NMR,ESI-MS.
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