BMS-275183的发现：一种口服有效的新型紫杉烷。
The discovery of BMS-275183: an orally efficacious novel taxane.
作者信息
Mastalerz Harold, Cook Donald, Fairchild Craig R, Hansel Steven, Johnson Walter, Kadow John F, Long Byron H, Rose William C, Tarrant James, Wu Mu-Jen, Xue May Quifen, Zhang Guifen, Zoeckler Mary, Vyas Dolatrai M
机构信息
Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, PO Box 5100, Wallingford, CT 06492-7660, USA.
出版信息
Bioorg Med Chem. 2003 Oct 1;11(20):4315-23. doi: 10.1016/s0968-0896(03)00495-4.
The evolution of 2, a C-4-methylcarbonate analogue of paclitaxel with minimal oral bioavailability and oral efficacy, into its C-3'-t-butyl-3'-N-t-butyloxycarbonyl analogue (15i), a novel taxane with oral efficacy in preclinical models that is comparable to iv administered paclitaxel, is described.
描述了2（一种口服生物利用度和口服疗效极低的紫杉醇C-4-甲基碳酸酯类似物）演变成其C-3'-叔丁基-3'-N-叔丁氧羰基类似物（15i）的过程，15i是一种在临床前模型中具有口服疗效且与静脉注射紫杉醇相当的新型紫杉烷。
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