Substituted quinolines for the treatment of cancer

121 2r2s 2r2s2t132 11 23323 2232s3221 2 Compounds of formula G-L-G, where -Gis a radical structurally close to cryptolepine, -L- is a single covalent bond or a covalent linking biradical selected from (CH)NR′″(CH)and -(CH)NR′″(CH)NR″″(CH)-, -R′″ and -R″″ are radicals, same or different, selected fro...

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Hauptverfasser: Bofarull, Juan Aymami, Capella, Miquel Coll, Soldevila, Amadeo Llebaria, Muñoz, Isabel Navarro
Format: Patent
Sprache:eng
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Zusammenfassung:121 2r2s 2r2s2t132 11 23323 2232s3221 2 Compounds of formula G-L-G, where -Gis a radical structurally close to cryptolepine, -L- is a single covalent bond or a covalent linking biradical selected from (CH)NR′″(CH)and -(CH)NR′″(CH)NR″″(CH)-, -R′″ and -R″″ are radicals, same or different, selected from the group consisting of H and (C-C)-alkyl; r, s and t are an integer from 1 to 3 and, -Gis H or a radical structurally close to -G, 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 -Gis bonded to -L- through a carbonyl amino and -L- is -(CH)NCH(CH)or -(CH)NCH(CH)NCH(CH)- where s =2 or 3. -Gis a radical selected from (IIa) y (IIb); -Gis 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.