Substituted 2-arylbenzazole compounds and their use as...

C - Chemistry – Metallurgy – 07 – D

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C07D 277/66 (2006.01) A61K 31/423 (2006.01) A61K 31/428 (2006.01) A61K 51/04 (2006.01) A61P 35/00 (2006.01) C07D 263/57 (2006.01) C07D 277/64 (2006.01)

Patent

CA 2382406

Substituted 2-phenylbenzazole compounds of formula (I) wherein X represents S or O and Q represents a direct bond, -CH2- or -CH=CH-, exhibit selective antiproliferative activity in respect of mammalian tumour cells. At least in preferred embodiments the benzene ring of the benzazole nucleus has a halogen substituent, preferably fluorine, and the 2-phenyl group has a 4'-amino substituent which may be conjugated with an amino acid to provide a water soluble amino acid amide prodrug or salt thereof.

L'invention concerne des composés 2-phénylbenzazole substitués représentés par la formule (I). Dans ladite formule, X est S ou O et Q est une liaison directe, -CH2- ou -CH=CH-. Ces composés ont une activité antiproliférative sélective vis-à-vis des cellules tumorales mammaliennes. Au moins en mode de réalisation préféré, la chaîne benzène du noyau benzazole comporte un substituant halogène, de préférence fluor, et le groupe 2-phényle présente un substituant 4'-amino susceptible d'être conjugué avec un acide aminé pour constituer un promédicament amide aminoacide hydrosoluble ou un sel correspondant.

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