Bis-(substituted-phenyl) derivatives with cytotoxic and...

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 233/80 (2006.01) A61K 31/16 (2006.01) A61K 31/21 (2006.01) A61K 31/415 (2006.01) C07C 233/62 (2006.01) C07C 237/40 (2006.01) C07C 279/12 (2006.01) C07C 311/46 (2006.01) C07C 323/37 (2006.01) C07D 231/14 (2006.01)

Patent

CA 2138389

The invention relates to novel polybenzamide mustards having anticancer and hypoxia-selective properties, to methods of preparing the novel compounds, and to the use of these compounds as anticancer agents. The compounds have general formula (I), wherein M and M1 separately represent H, aziridinyl, N(Et)CH2CH2Y or N(CH2CH2Y)2, where Y is Cl, Br, I or OSO2Me; R and R1 separately represent up to three of H, NO2, aza (ring CH= replaced by N=), CH2Q, SO2NHQ or CONHQ, where Q is H, Me, (CH2)nNMe2, (CH2)nNHC(= NH)NH2 and n = 2-4); X represents CONH, NHCO, O, CH2, NH or S; and A is (CH2)n, where n = 2 to 4, or a unit chosen from formulae (IIa to IIc) wherein Z = CH2Q, SO2NHQ or CONHQ, where Q is H, Me, (CH2)nNMe2, (CH2)nNHC(= NH)NH2 and n = 2 to 4), or an acid addition salt or N-oxide thereof.

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