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2004
Triazole derivatives
R 0280
Synthesis and Antiproliferative Activity of 3-Aryl-2-[1H(2H)-benzotriazolVariously Substituted. Part 4. — Two new series of benzotri47- 123 -1(2)-yl]acrylonitriles
azolyl acrylonitriles like (VI) and (XII) are prepared by condensation of benzotriazoles
(I) and (VII) with chloroacetonitrile (II). The N-alkylated products are obtained as mixtures of isomers. In the first series, the effect of electron-releasing or electron-withdrawing groups associated with the increase of lipophilicity and steric hindrance on antiproliferative activity is investigated, while in the second series, the influence of substituents at the phenyl moiety, found active against M. tuberculosis, are examined. The
syntheses are accomplished by Knoevenagel condensation of the intermediates with
appropriate aldehydes, e.g. (V). The most cytotoxic compounds are evaluated against
a panel of human cell lines derived from hematological and solid tumors. Compound
(VI) is more potent than 6-mercaptopurine on all cell lines, but less potent than etoposide. Compounds (XI) and (XII) display moderate activity against some resistant strains
of Mycobacterium. — (CARTA*, A.; PALOMBA, M.; BOATTO, G.; BUSONERA,
B.; MURREDDU, M.; LODDO, R.; Farmaco 59 (2004) 8, 637-644; Dip. Farm.
Chim. Tossicol., Univ. Sassari, I-07100 Sassari, Italy; Eng.) —
H. Hoennerscheid
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