Cytotoxic quinolines (part 1). Azolylalkyloxy quinolines and 1-azolylalkyl-4(1H)-quinolones

A series of 4-azolylalkyloxyquinolines and 1-azolylalkyl-4(1H)-quinolones has been synthesized and evaluated for cytotoxicity against various cancer cell lines. 1-Phenyl-1,2,3-triazole and 1-methylpyrazole were found to be the most effective azoles. The length of the alkyl chain was critical, with 8...

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Bibliographic Details
Published inDrug design and discovery Vol. 14; no. 1; p. 15
Main Authors Abel, M D, Ha, C M, Luu, H T, Micetich, R G, Nguyen, D Q, Nukatsuka, M, Oreski, A B, Tempest, M L, Daneshtalab, M
Format Journal Article
LanguageEnglish
Published Switzerland 01.03.1996
Subjects
Animals
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Azo Compounds - chemistry
DNA - chemistry
Drug Screening Assays, Antitumor
Humans
Oxyquinoline - chemistry
Quinolines - chemistry
Quinolines - pharmacology
Tumor Cells, Cultured - drug effects
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Summary:A series of 4-azolylalkyloxyquinolines and 1-azolylalkyl-4(1H)-quinolones has been synthesized and evaluated for cytotoxicity against various cancer cell lines. 1-Phenyl-1,2,3-triazole and 1-methylpyrazole were found to be the most effective azoles. The length of the alkyl chain was critical, with 8 to 10 carbon atoms being optimal. Several of the compounds were found to be very cytotoxic in vitro towards various cancer cells. Compounds 9o, 10k, and 10r were evaluated in vivo, but were ineffective and exhibited acute general toxicity at higher dosages.
ISSN:1055-9612