Importance

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Abstract

Compounds of formula G₁-L-G₂, where G₁, is a radical structurally close to cryptolepine, -L- is a single covalent bond or a covalent linking biradical selected from —(CH₂)_rNR′″(CH₂)_s— and —(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 -G₂ is 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 citotoxicity with human leukemia cells Jurkat E6-1 and human carcinoma cells GLC-4. Preferred compounds are those where -G₁ is bonded to -L- through a carbonyl amino and -L- is —(CH₂)₃NCH₃(CH₂)₃— or —(CH₂)₂NCH₃(CH₂)_sNCH₃(CH₂)₂— where s=2 or 3.-G₁ is a radical selected from (IIa) and (IIb); -G₂ is 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.

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First Claim