Abstract
Some tetracyclic quinolines (9 and 14) with a [2-methoxy-4-[(methylsulfonyl)amino]phenyl]amino side chain were prepared and their deoxyribonucleic acid (DNA) intercalative properties, KB cytotoxicity, antitumor activity (P388 leukemia), and ability to induce topoisomerase II dependent DNA cleavage were investigated. The indoloquinoline derivative 9 exhibited the most potent activity (dose = 6.3 mg, T/C% = 300) in this series. The steric structural features of the chromophores of the compounds previously and newly synthesized were studied by a computer-associated molecular graphics technique. Relationships between the steric structural features of the chromophores and biological activities are also discussed.
Original language | English |
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Pages (from-to) | 3048-3052 |
Number of pages | 5 |
Journal | Chemical and Pharmaceutical Bulletin |
Volume | 38 |
Issue number | 11 |
DOIs | |
Publication status | Published - 1990 |
Keywords
- antitumor activity
- indoloquinoline
- intercalation
- molecular graphics
- synthesis
- topoisomerase II
ASJC Scopus subject areas
- Chemistry(all)
- Drug Discovery