海鞘素光亲和类似物的合成与生物学评价

Synthesis and biological evaluation of didemnin photoaffinity analogues.

作者信息

Vera M D, Pfizenmayer A J, Ding X, Ahuja D, Toogood P L, Joullié M M

机构信息

Department of Chemistry, University of Pennsylvania, 19104-6323, Philadelphia, PA, USA.

出版信息

Bioorg Med Chem Lett. 2001 Jul 23;11(14):1871-4. doi: 10.1016/s0960-894x(01)00339-0.

DOI:10.1016/s0960-894x(01)00339-0

PMID:11459650

Abstract

The synthesis of four benzophenone-containing analogues of the antiproliferative natural product didemnin B is presented. In vitro protein biosynthesis inhibition potency and antitumor activity were evaluated. The results indicate that all four analogues are biologically active and could serve as photoaffinity reagents for the study of receptor-binding interactions of didemnins. These analogues could also be useful in studying antitumor effects of didemnins.

摘要

本文介绍了抗增殖天然产物didemnin B的四种含二苯甲酮类似物的合成。评估了其体外蛋白质生物合成抑制效力和抗肿瘤活性。结果表明，所有四种类似物均具有生物活性，可作为光亲和试剂用于研究didemnins的受体结合相互作用。这些类似物也可用于研究didemnins的抗肿瘤作用。