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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Authors | D 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 |
Journal | Bioorganic & medicinal chemistry letters
(Bioorg Med Chem Lett)
Vol. 9
Issue 3
Pg. 369-74
(Feb 08 1999)
ISSN: 0960-894X [Print] England |
PMID | 10091686
(Publication Type: Journal Article)
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Chemical References |
- Antineoplastic Agents
- Depsipeptides
- Peptides, Cyclic
- cryptophycin
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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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