细胞毒性简化的微管溶素类似物

Cytotoxic simplified tubulysin analogues.

作者信息

Raghavan Bhooma, Balasubramanian Ranganathan, Steele Jaeson C, Sackett Dan L, Fecik Robert A

机构信息

Department of Medicinal Chemistry. 308 Harvard Street SE, University of Minnesota, Minneapolis, MN 55455, USA.

出版信息

J Med Chem. 2008 Mar 27;51(6):1530-3. doi: 10.1021/jm701321p. Epub 2008 Mar 4.

DOI:10.1021/jm701321p

PMID:18314944

Abstract

An efficient route for the synthesis of the tubulysin family of antimitotic peptides was developed. Simplified tubulysin analogues were synthesized to define the minimum pharmacophore required for cytotoxicity. Simplified tubulysin analogues retain significant cytotoxicity and reveal important preliminary structure-activity relationships.

摘要

开发了一种合成抗有丝分裂肽tubulysin家族的有效途径。合成了简化的tubulysin类似物以确定细胞毒性所需的最小药效团。简化的tubulysin类似物保留了显著的细胞毒性，并揭示了重要的初步构效关系。