title: 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.
authors: Lilly Research Laboratories, A Division of Eli Lilly and Co., Indianapolis, IN 46285, USA.
authors: D L
authors: DL
authors: Varie
authors: C
authors: C
authors: Shih
authors: D A
authors: DA
authors: Hay
authors: S L
authors: SL
authors: Andis
authors: T H
authors: TH
authors: Corbett
authors: L S
authors: LS
authors: Gossett
authors: S K
authors: SK
authors: Janisse
authors: M J
authors: MJ
authors: Martinelli
authors: E D
authors: ED
authors: Moher
authors: R M
authors: RM
authors: Schultz
authors: J E
authors: JE
authors: Toth
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D047630:Depsipeptides; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D051379:Mice; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D047630:Depsipeptides; D010456:Peptides, Cyclic; C088419:cryptophycin