Design of antineoplastic agents based on the '2-phenylnaphthalene-type' structural pattern. 4. Synthesis and biological activity of 2-chloro-3- (substituted phenoxy)-1,4-naphthoquinones and related 5,8-dihydroxy-1,4- naphthoquinones

He Xi Chang, Ting Chao Chou, Niramol Savaraj, Leroy F. Liu, Chiang Yu, C. C. Cheng

Research output: Contribution to journalArticle

41 Scopus citations


The intermediate in the preparation of 1,3,7,10- tetrahydroxybenzo[b]naphtho[2,3-d]furan-6,11-dione (2), 2-chloro-5,8- dimethoxy-3-(3,5-dimethoxyphenoxy)-1,4-naphthoquinone (8h), and corresponding hydroxyl, methoxyl, and acetoxyl analogues was found to possess interesting inhibitory activities in a number of cytotoxic test systems. Activities were also noticed in some 5,8-dihydroxy-1,4-naphthoquinone derivatives. A structure-activity discussion of compounds of this series is presented. The newly uncovered biological activity of 2-chloro-3-(substituted phenoxyl)- 1,4-naphthoquinones and 2,3-bis(substituted phenoxy)-1,4-naphthoquinones may suggest an approach for the development of new classes of antineoplastic agents.

Original languageEnglish
Pages (from-to)405-408
Number of pages4
JournalJournal of Medicinal Chemistry
Issue number3
StatePublished - Feb 24 1999


ASJC Scopus subject areas

  • Organic Chemistry

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