首页> 外国专利> Vinblastine 20'amide: a synthetic analog that maintains or improves potency while overcoming Pgp-derived efflux and resistance

Vinblastine 20'amide: a synthetic analog that maintains or improves potency while overcoming Pgp-derived efflux and resistance

机译:长春碱20'酰胺:一种合成类似物,可维持或提高效力,同时克服Pgp衍生的外排和抵抗力

摘要

A vinca alkaloid compound substituted at the 20′-position with a carboxamido group is disclosed. The carbonyl of the carboxamido group is bonded to a 20′-amino group and to a ring system that contains up to three 5-, 6- or 7-membered rings that are fused or otherwise bonded together. Each ring can be carbocyclic or heterocyclic, with a heterocyclic ring containing up to three hetero ring atoms that are the same or different and are selected from nitrogen, oxygen and sulfur. The ring system can include up to four substituent groups other than hydrogen that are discussed within. Methods of preparing the compounds are disclosed as are compositions for their use and methods of treatment using d compound. A particularly preferred compound has an activity in specified cancer cell growth inhibition assays that is the same or better than its parental, unsubstituted vinca compound and is not subject to Pgp-mediated efflux.
机译:公开了在20'-位被羧酰胺基取代的长春花生物碱化合物。羧酰胺基的羰基键合至20'-氨基和环系统,该环系统包含最多三个稠合或以其他方式键合的5、6或7元环。每个环可以是碳环或杂环,其中杂环含有至多三个相同或不同并且选自氮,氧和硫的杂环原子。环系统可包含除氢以外的多达四个取代基。公开了制备化合物的方法以及其用途的组合物和使用d化合物的治疗方法。特别优选的化合物在特定的癌细胞生长抑制试验中具有与其母体未取代的长春花化合物相同或更好的活性,并且不经受Pgp介导的外排。

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