Design of Antineoplastic Agents on the Basis of the “2-Phenylnaphthalene-Type” Structural Pattern. 2. Synthesis and Biological Activity Studies of Benzo[A]naphtho[2,3-d]furan-6,11-dione Derivatives

C. C. Cheng, Qing Dong, Dun Fu Liu, Yi Lin Luo, Leroy F. Liu, Allan Y. Chen, Chiang Yu, Niramol Savaraj, Ting Chao Chou

研究成果: 雜誌貢獻文章同行評審

59 引文 斯高帕斯(Scopus)

摘要

Based on the “2-phenylnaphthalene-type” structural pattern hypothesis developed in our laboratory, a number of benzo[b]naphtho[2,3-d]furan-6,11-diones were designed, synthesized, and evaluated in vitro for their inhibitory action against the growth of human promyelocytic leukemia cells (HL-60), small-cell lung cancer (SCLC), SCLC cells resistant to cisplatin (SCLC/CDDP), National Cancer Institute's disease-oriented primary antitumor 60 cell-line panel, and drug-stimulated topoisomerase II-mediated DNA cleavages. Many compounds designed were found to possess potent activity in one or more of the biological tests. In general, activity found in one of the cell lines tested is often echoed in other cell lines and many also expressed substantial inhibitory activity against topoisomerase II-mediated cleavage activities. One of these compounds, 3-[2-(dimethylamino)ethoxy]-1-hydroxybenzo[b]naphtho[2,3-d]furan-6,11-dione (8j), exhibited strong inhibitory activity throughout the entire series of test panel. Thus, it appears that the proposed structural pattern hypothesis has received substantial support through experimental verification.

原文英語
頁(從 - 到)4108-4112
頁數5
期刊Journal of Medicinal Chemistry
36
發行號25
DOIs
出版狀態已發佈 - 1993

ASJC Scopus subject areas

  • 分子醫學
  • 藥物發現

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