Ring-Hydroxylated Analogues of Lucanthone as Antitumor Agents

Sydney Archer, Kenneth J. Miller, Rabindra Rej, Cecily Periana, Lloyd Fricker

Research output: Contribution to journalArticle

29 Scopus citations

Abstract

A series of ring-alkoxylated and ring-hydroxylated analogues of lucanthone was prepared and tested for antitumor activity. The most biologically interesting members of this group were the 7-hydroxylucanthone derivatives, 50 and 51, which gave T/C values in the NCI P-388 antitumor screen of 188 and 265, respectively. The apparent association constants and ΔTm values for a number of analogue-DNA complexes were determined to ascertain whether there was any quantitative correlation with biological activity. The most that can be said is that intercalation may be a necessary but far from sufficient condition for antitumor activity.

Original languageEnglish (US)
Pages (from-to)220-227
Number of pages8
JournalJournal of Medicinal Chemistry
Volume25
Issue number3
DOIs
StatePublished - Jan 1 1982

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ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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