Synthesis and biological evaluation of cryptophycin analogs with substitution at C-6 (fragment C region) |
| |
| Authors: | Varie D L Shih C Hay D A Andis S L Corbett T H Gossett L S Janisse S K Martinelli M J Moher E D Schultz R M Toth J E |
| |
| Institution: | Lilly Research Laboratories, A Division of Eli Lilly and Co., Indianapolis, IN 46285, USA. |
| |
| Abstract: | Analogs of the antitumor agents cryptophycins 1 and 8 with dialkyl substitution at C-6 (fragment C) were synthesized and evaluated for in vitro cytotoxicity against human leukemia cells (CCRF-CEM). The activity of these analogs decreased as the size of the substituents at C-6 increased. The C-6 spirocylopropyl compound (2g) was highly potent in vitro and showed excellent antitumor activity in animal models. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ |
