Substituted quinolines for the treatment of cancer

Details Substituted quinolines for the treatment of cancer Substituted quinolines for the treatment of cancer

2004-11-18

2010-06-01

Aulakh, Charanjit S (Department: 1625)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

C546S062000

Reexamination Certificate

active

07728000

ABSTRACT:
Compounds of formula G1-L-G2, where -G1is a radical structurally close to cryptolepine, -L- is a single covalent bond or a covalent linking biradical selected from (CH2)rNR′″(CH2)sand —(CH2)rNR′″(CH2)sNR″″(CH2)t—, —R′″ and —R″″ are radicals, same or different, selected from the group consisting of H and (C1-C3)-alkyl; r, s and t are an integer from 1 to 3 and, -G2is H or a radical structurally close to -G1, are intercalators. They are compounds which intercalate between DNA base pairs, and are useful as therapeutic agents against cancer, as assess by an in vitro test of cytotoxicity with human leukemia cells Jurkat E6-1 and human carcinoma cells GLC-4. Preferred compounds are those where -G1is bonded to -L- through a carbonyl amino and -L- is —(CH2)3NCH3(CH2)3or —(CH2)2NCH3(CH2)sNCH3(CH2)2— where s =2 or 3. -G1is a radical selected from (IIa) y (IIb); -G2is a radical selected from H, a radical of formula (IIa), a radical of formula (IIb), the N-radical of 1,8-naphthalimide, the C4-radical of 2-phenylquinoline, and the C9-radical of acridine.

REFERENCES:
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