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

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.
AuthorsD L Varie, C Shih, D A Hay, S L Andis, T H Corbett, L S Gossett, S K Janisse, M J Martinelli, E D Moher, R M Schultz, J E Toth
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 9 Issue 3 Pg. 369-74 (Feb 08 1999) ISSN: 0960-894X [Print] England
PMID10091686 (Publication Type: Journal Article)
Chemical References
  • Antineoplastic Agents
  • Depsipeptides
  • Peptides, Cyclic
  • cryptophycin
Topics
  • Animals
  • Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
  • Depsipeptides
  • Drug Screening Assays, Antitumor
  • Humans
  • Mice
  • Peptides, Cyclic (chemical synthesis, chemistry, pharmacology)
  • Tumor Cells, Cultured

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