Quinoline derivatives having anti-tumor activity

Details Quinoline derivatives having anti-tumor activity Quinoline derivatives having anti-tumor activity

1990-09-17

1992-05-12

Daus, Donald G.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514311, 514513, 514314, 514 15, 514 16, 514 17, 514 18, 514 19, 546153, 546155, 546162, 546176, 546161, 546169, 546180, 530327, 530328, 530329, 530330, 530331, 530332, A61K 3147, C07D21500

Patent

active

051128373

ABSTRACT:
The invention relates to a quinoline of the formula: ##STR1## wherein each of R.sup.1 and R.sup.2, which may be the same or different, is hydrogen, halogeno, hydroxy, cyano, carbamoyl, nitro or amino, alkyl, alkoxy, alkylthio, alkylamino, dialkylamino or alkanoylamino each of up to 4 carbon atoms, or substituted alkyl or alkoxy each of up to 3 carbon atoms, provided that both R.sup.1 and R.sup.2 are not hydrogen; the quinoline ring may bear further substituents; R.sup.3 is hydrogen or alkyl of up to 4 carbon atoms; R.sup.4 is hydrogen, alkyl, alkenyl or alkynyl each of up to 4 carbon atoms or substituted alkyl of up to 3 carbon atoms; Ar is phenylene, naphthylene or heterocyclene which is unsubstituted or which bears one or more substituents; R.sup.5 is such that R.sup.5 --NH.sub.2 is an amino acid; or a pharmaceutically-acceptable salt or ester thereof. The compounds possess anti-tumor activity.

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Burger, "Medicinal Chemistry" 2d. Ed., Interscience, New York, 1960, p. 42,497.

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