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 language | English (US) |
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Pages (from-to) | 220-227 |
Number of pages | 8 |
Journal | Journal of Medicinal Chemistry |
Volume | 25 |
Issue number | 3 |
DOIs | |
State | Published - 1982 |
Externally published | Yes |
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery