- Effect of side chain location in (2-aminoethyl)aminomethyl-2- phenylquinolines as antitumor agents
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Three new derivatives of 2-phenylquinoline having an (2- aminoethyl)aminomethyl group in 7-, 6-, or 4'-(para position of 2-phenyl ring) positions of aromatic system have been prepared. The antitumor activity of these compounds together with 8- or 4- substituted isomers against the HeLa cell is in the order of 8- > 7- > 4- ? 6- ? 4'- substituted ones, which is almost in good agreement with that of DNA-binding ability evaluated by means of DNA-titration of UV-VIS spectra, DNA melting experiment, and ethidium displacement assay. Two representative compounds (8- and 4- isomers) are confirmed to have an ability to intercalate into double stranded DNA by topoisomerase I superhelix unwinding assay.
- Mikata, Yuji,Yokoyama, Mika,Ogura, Shun-ichiro,Okura, Ichiro,Kawasaki, Masafumi,Maeda, Mizuo,Yano, Shigenobu
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- Quinolineacetic acid compositions
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Compounds of the formula SPC1 Wherein Ar denotes an optionally substituted phenyl group or hetero-aromatic group with 5 or 6 ring members wherein the atom directly bonded to the quinoline ring is a carbon atom, R1 represents hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl and R2 and R3 independently of one another denote hydrogen or a lower alkyl group, esters and amides of these carboxylic acids or salts of such compounds, have anti-inflammatory and analgesic activity; they are active ingredients of pharmaceutical compositions and can be used for the relief and removal of pain as well as for the treatment of rheumatic, arthritic and other inflammatory complaints; an illustrative example is α-methyl-2-(2-thienyl)-6-quinolineacetic acid.
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