Synthesis and pharmacological evaluation of isoindolo[1,2-b]quinazolinone and isoindolo[2,1-a]benzimidazole derivatives related to the antitumor agent batracylin

Sanath K. Meegalla, Gregory J. Stevens, Charlene A. McQueen, Allan Y. Chen, Chiang Yu, Leroy F. Liu, Louis R. Barrows, Edmond J. LaVoie

研究成果: 雜誌貢獻文章同行評審

40 引文 斯高帕斯(Scopus)

摘要

The synthesis and pharmacological activity of isoindolo[1,2-b]quinazolin-12(10H)-ones and isoindolo[2,1-a]benzimidazoles related to batracylin are described. The acute toxicity of batracyclin has been associated with the formation of its N-acetyl metabolite which is a potent inducer of unscheduled DNA synthesis in rat hepatocytes. The desamino derivative and the 8-aza analog of batracylin retained the ability to inhibit topoisomerase II but did not induce unscheduled DNA synthesis. While less active than batracylin, these analogs were cytotoxic to CCRF CEM leukemia cells. The isoindolo[2,1-a]benzimidazole derivatives were inactive as topoisomerase II inhibitors and, in general, failed to exhibit comparable antitumor activity or to induce unscheduled DNA synthesis.

原文英語
頁(從 - 到)3434-3439
頁數6
期刊Journal of Medicinal Chemistry
37
發行號20
出版狀態已發佈 - 1994
對外發佈

ASJC Scopus subject areas

  • 有機化學

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