Synthesis of 7-Epi (+)-FR900482:: An epimer of comparable anti-cancer activity
Synthesis of 7-Epi (+)-FR900482:: An epimer of comparable anti-cancer activity
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DOI：
10.1021/ol800127a
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发表时间：
2008-04-03
期刊：
影响因子：
5.2
通讯作者：
O'Boyle, Brendan M.
中科院分区：
文献类型：
--
作者：
Trost, Barry M.;O'Boyle, Brendan M.
FR 900482是一种有效的抗肿瘤治疗剂，已被研究作为临床有用的丝裂霉素C的替代候选物。在此，我们报告了7-Epi（+）-FR 900482的合成和生物学测试，其证明了相对于天然产物对几种癌细胞系的同等效力。这项工作的亮点包括利用我们的钯催化DYKAT方法和开发的Polonovski氧化环扩张策略，以产生这种等效差向异构体在23个线性步骤。
FR900482 is a potent anti-tumor therapeutic that has been investigated as a replacement candidate for the clinically useful Mitomycin C. Herein, we report synthesis and biological testing of 7-Epi (+)-FR900482, which demonstrates equal potency relative to the natural product against several cancer cell lines. Highlights of this work include utilization of our palladium-catalyzed DYKAT methodology and development of a Polonovski oxidative ring expansion strategy to yield this equipotent epimer in 23 linear steps.