1. Academic Validation
  2. Synthesis and topoisomerase poisoning activity of A-ring and E-ring substituted luotonin A derivatives

Synthesis and topoisomerase poisoning activity of A-ring and E-ring substituted luotonin A derivatives

  • Bioorg Med Chem. 2007 Jun 15;15(12):4237-46. doi: 10.1016/j.bmc.2007.03.067.
Kassoum Nacro 1 Conxiang Charles Zha Peter R Guzzo R Jason Herr Denise Peace Thomas D Friedrich
Affiliations

Affiliation

  • 1 Discovery Research & Development, Albany Molecular Research Inc., Albany, NY 12213-5098, USA.
Abstract

A series of A-ring and E-ring analogues of the natural product luotonin A, a known Topoisomerase I poison, was evaluated for growth inhibition in human carcinoma and leukemia cell lines. Rational design of structures was based on analogues of the related alkaloid camptothecin, which has been demonstrated to exert cytotoxic effects by the same mechanism of action. When compared to luotonin A, several compounds exhibited an improved Topoisomerase I-dependent growth inhibition of a human leukemia cell line.

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