Thioanalogues of anti-tumor antibiotics. II. Synthesis and preliminary in vitro cytotoxicity evaluation of tricyclic [1,4]benzothiazepine derivatives

A. Garofalo, G. Balconi, M. Botta, F. Corelli, M. D'Incalci, G. Fabrizi, I. Fiorini, D. Lamba, V. Nacci

Research output: Contribution to journalArticle

Abstract

The synthesis of tricyclic [1,4]benzothiazepine derivatives starting from optically active cyclic amino acids and amino alcohols is described. The absolute configurations of the target compounds were assigned by X-ray and 1H-NMR analyses and by molecular modeling studies. The cytotoxic activity of the tricyclic derivatives was tested in vitro by growth inhibition assays using murine L1210 and human lymphoblastic CCRF-CEM leukemias. Compounds 5, 9, and 10 exhibited marked cytotoxic activity.

Original languageEnglish
Pages (from-to)213-220
Number of pages8
JournalEuropean Journal of Medicinal Chemistry
Volume28
Issue number3
DOIs
Publication statusPublished - 1993

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Keywords

  • 1,4-benzothiazepine
  • cytotoxicity
  • l-thioproline
  • leukemia L1210

ASJC Scopus subject areas

  • Molecular Medicine
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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