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Abstract

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Paper | Special issue | Vol 35, No. 2, 1993, pp. 775 - 789
Published online:
DOI: 10.3987/COM-92-S(T)51
Design of Antineoplastic Agents on the Basis of the "2-Phenylnaphthalene-Type" Structural Pattern. I. Synthesis of Substituted 3-Phenylquinazolones, Benzoxazolo[2,3-b]quinazolones and Benzothiazolo[2,3-b]quinazolones

Chia-Chung Cheng,* Dun-Fu Liu, and Ting Chao Chou

*Drug Development Laboratory, The University of Kansas Cancer Center and Department of Pharmacology, Toxicology & Therapeutics, The University of Kansas Medical Center, Kansas City, Kansas 66160-7419, U.S.A.

Abstract

A number of substituted 3-phenylquinazolin-4-ones, 12H-benzoxazolo[2,3-b]quinazolin-12-ones and 12H-benzothiazolo[2,3-b]quinazolin-12-ones designed and synthesized on the basis of a “2-phenylnaphthalene-type” structural pattern hypothesis. The postulated pattern, which was uncovered among a substantial number of compounds of both natural and synthetic origins, was noted to be associated with compounds possessing a variety of biological properties which include the antineoplastic activity. Several compounds designed for the present study were found to exhibit potent cytotoxicity against the growth of human promyelocytic leukemia (HL-60) cells.

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