2. Academic Validation
  3. Novel cyclopropapyrroloindole derivative (AT-3510) bearing methoxycarbonyl and trifluoromethyl groups

Novel cyclopropapyrroloindole derivative (AT-3510) bearing methoxycarbonyl and trifluoromethyl groups

  • J Med Chem. 1999 Apr 22;42(8):1448-58. doi: 10.1021/jm980668c.
Y Fukuda 1,  H Furuta,  Y Kusama,  H Ebisu,  Y Oomori,  S Terashima
Affiliations

Affiliation

  • 1 Central Research Laboratories, Kyorin Pharmaceutical Company Ltd., Mitarai, Nogi, Tochigi 329-0114, Japan.
PMID: 10212131 DOI: 10.1021/jm980668c
Abstract

The seco-Cl 3-methoxycarbonyl-2-trifluoromethylcyclopropapyrroloindole (MCTFCPI) derivatives dl- and/or (S)-10 carrying various acyl moieties at the N6-position were synthesized along with their prodrugs (S)-12, and their antitumor activity was evaluated. Among these derivatives, AT-3510 [(S)-12m], the novel prodrug MCTFCPI derivative carrying a 5-(7-methoxybenzofuran-2-ylcarbonyl)aminoindole-2-carb onyl group at the N6-position, was found to exhibit more excellent antitumor activity against human tumor xenografts than the clinical trial candidates carzelesin (6) and KW-2189 (7) and cisplatin.

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