Novel water-soluble c-ring analogues of 20 (s)-camptothecin

Details Novel water-soluble c-ring analogues of 20 (s)-camptothecin Novel water-soluble c-ring analogues of 20 (s)-camptothecin

C - Chemistry, Metallurgy

07

D

C07D 491/22 (2006.01) A61K 31/47 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01)

Patent

CA 2228595

Novel water-soluble C-ring analogues of 20(S)-camptothecin having general formula (1). All the compounds of formula (I) are prepared from the compounds of general formula (2) having 20(S)-chiral carbon where R1 to R5 have the meaning given above. The compounds of formula (1) possess potent anti-cancer and anti-viral properties. The invention also provides an alternate process for the preparation of known C-5 substituted compounds of formula (1).

Nouveaux analogues de noyaux C hydrosolubles de 20(S)-camptothécine ayant la formule générale (1). Tous les composés de la formule (1) sont préparés à aprtir des composés de la formule générale (2) présentant un carbone 20(S)-chiral dans laquelle R<1> à R<5> ont la notation donnée dans la description. Les composés de la formule (1) présentent des propriétés anticancéreuses et antivirales puissantes. L'invention concerne également un autre procédé de préparation de composés à substitution C-5 connus de la formule (1).

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