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Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
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Synthesis and biological evaluation of cryptophycin analogs with substitution at C-6 (fragment C region)
1Lilly Research Laboratories, A Division of Eli Lilly and Co., Indianapolis, IN 46285, USA.
Bioorganic & Medicinal Chemistry Letters
|March 26, 1999
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.
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