Solid‐phase Total Synthesis of Amide Analogues of Coibamide A: Azacoibamide A and O‐Desmethyl Azacoibamide A
[摘要] Solidâphase total syntheses of highly methylated cyclic azacoibamide A and its Oâdesmethyl analogue were achieved. Two ester linkages of natural coibamide A were replaced by amide bonds to improve its pharmacokinetic properties. The synthetic strategy consists of the key onâresin macrocyclization, N,Nâdimethylation, and final solution phase Oâmethylation reactions. Compared to the naturally occurring coibamide A, azacoibamide A and its Oâdesmethyl analogue displayed low micromolar activities against tested cancer cell lines.
[发布日期] [发布机构]
[效力级别] [学科分类] 化学（综合）
[关键词] Solid‐phase synthesis;Coibamide A;Azacoibamide A;On‐resin cyclization;O‐Methylation [时效性]
