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 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.
Abel
M D
MD
SynPhar Laboratories Inc., Edmonton Alberto, Canada.
Ha
C M
CM
Luu
H T
HT
Micetich
R G
RG
Nguyen
D Q
DQ
Nukatsuka
M
M
Oreski
A B
AB
Tempest
M L
ML
Daneshtalab
M
M
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D001391:Azo Compounds / Q000737:chemistry*; D004247:DNA / Q000737:chemistry; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015125:Oxyquinoline / Q000737:chemistry*; D011804:Quinolines / Q000737:chemistry* / Q000494:pharmacology; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000970:Antineoplastic Agents; D001391:Azo Compounds; D011804:Quinolines; D015125:Oxyquinoline; D004247:DNA