Synthesis and biological evaluation of cryptophycin analogs with substitution at C-6 (fragment C region)

Authors
Varie, DL Shih, C Hay, DA Andis, SL Corbett, TH Gossett, LS Janisse, SK Martinelli, MJ Moher, ED Schultz, RM Toth, JE
Citation
Dl. Varie et al., Synthesis and biological evaluation of cryptophycin analogs with substitution at C-6 (fragment C region), BIOORG MED, 9(3), 1999, pp. 369-374
Citations number
17
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
3
Year of publication
1999
Pages
369 - 374
Database
ISI
SICI code
0960-894X(19990208)9:3<369:SABEOC>2.0.ZU;2-1
Abstract
Analogs of the antitumor agents cryptophycins 1 and 8 with dialkyl substitu tion at C-6 (fragment C) were synthesized and evaluated for in vitro cytoto xicity against human leukemia cells (CCRF-CEM). The activity of these analo gs decreased as the size of the substituents at C-6 increased. The C-6 spir ocylopropyl compound (2g) was highly potent in vitro and showed excellent a ntitumor activity in animal models. (C) 1999 Elsevier Science Ltd. ALI righ ts reserved.