Design of new topoisomerase II inhibitors based upon a quinobenzoxazine self-assembly model

Qingping Zeng, Yan Kwok, Sean M. Kerwin, Gina Mangold, Laurence H. Hurley

Research output: Contribution to journalArticlepeer-review

37 Scopus citations

Abstract

A new class of pyridobenzophenoxazine compounds has been developed as topoisomerase II inhibitors for anticancer chemotherapy. These compounds were designed based on a proposed model of a quinobenzoxazine self-assembly complex on DNA. They showed excellent inhibitory effects on several tumor cell lines with nanomolar IC50 values. Their cytotoxic potency correlates with theft ability to unwind DNA and inhibit topoisomerase II.

Original languageEnglish (US)
Pages (from-to)4273-4278
Number of pages6
JournalJournal of Medicinal Chemistry
Volume41
Issue number22
DOIs
StatePublished - Oct 23 1998
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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