Camptothecin derivatives and the use thereof as antitumor...

Details Camptothecin derivatives and the use thereof as antitumor... Camptothecin derivatives and the use thereof as antitumor...

C - Chemistry, Metallurgy

07

D

C07D 491/22 (2006.01) A61K 31/47 (2006.01) A61K 31/4745 (2006.01) A61K 31/70 (2006.01) C07H 15/26 (2006.01)

Patent

CA 2247513

Compounds of formula (I), wherein: R1 is -CN, -CH(CN)-R4, -CH=C(CN)-R4, -CH2- CH(CN)-R4, -C(=NOH)-NH2, -C(=NH)-NH2, -CH-C(NO2)-R4, -CH(CN)-R5, -CH(CH2NO2)-R5; 5-tetrazolyl, 2-(4,5-dihydrooxazolyl), 1,2,4- oxadiazolin-3-yl-5-one; R2 is hydrogen; R3 is hydrogen, OR6; R4 is hydrogen, C1-C6 linear or branched alkyl, CN, COOR7; R5 is hydrogen, OR8; R6 is hydrogen, C1-C6 linear or branched alkyl, (C6-C12) aryl (C1-C4) alkyl, (C1-C4) alkoxy (C1-C4) alkyl, (C1-C4) alkyl (C6-C12) aryl, (C6-C12) aryl (C2-C4) acyl, (C2-C4) acyl, amino (C1-C4) alkyl, amino (C2-C4) acyl, glycosyl; R7 is hydrogen, C1-C6 linear or branched alkyl, (C6-C12) aryl (C1-C4) alkyl, (C1-C4) alkoxy (C1-C4) alkyl, (C1-C4) alkyl (C6-C12) aryl; R8 has the same meanings of R6, independently of the latter. These compounds are active as topoisomerase I inhibitors and can be used as antitumor drugs.

L'invention concerne des composés présentant la formule (I), dans laquelle R1 est -CN, -CH(CN)-R4, -CH=C(CN)-R4, -CH2-CH(CN)-R4, -C(=NOH)-NH2, -C(=NH)-NH2, -CH=C(NO2)-R4, -CH(CN)-R5, -CH(CH2NO2)-R5; 5-tétrazolyl, 2-(4,5-dihydrooxazolyl), 1,2,4-oxadiazolin-3-yl-5-one; R2 est hydrogène; R3 est hydrogène, OR6; R4 est hydrogène, alkyle C1-C6 linéaire ou ramifié, CN, COOR7; R5 est hydrogène; OR8; R6 est hydrogène; alkyle C1-C6 linéaire ou ramifié, aryle (C6-C12) alkyle (C1-C4), alkoxy (C1-C4) alkyle (C1-C4), alkyle (C1-C4) aryle (C6-C12), aryle (C6-C12) acyle (C2-C4), acyle (C2-C4), alkyle (C1-C4) aminé, acyle (C2-C4) aminé, glycosyle; R7 est hydrogène, alkyle C1-C6 linéaire ou ramifié, aryle (C6-C12) alkyle (C1-C4), alkoxy (C1-C4) alkyle (C1-C4), alkyle (C1-C4) aryle (C6-C12); R8 a la même signification que R6, indépendamment de ce dernier. Ces composés sont actifs comme inhibiteurs de la topo-isomérase I et peuvent être utilisés comme produits antitumoraux.

Affiliated with

Also associated with

Rating

Camptothecin derivatives and the use thereof as antitumor... does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Camptothecin derivatives and the use thereof as antitumor..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Camptothecin derivatives and the use thereof as antitumor... will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFCA-PAI-O-1868610