Hydroxamic acid dervicatives as inhibitors of hdac enzymatic activity
作者： Sanjay Ratilal Patel , David Festus Charles Moffat , Alan Hornsby Davidson
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摘要: Compounds of formula (I) are inhibitors histone deacetylase activity, and useful in the treatment of, for example, cancers: wherein Y1 is a bond, -(C=O)-, -S(O2)-, -C(=O)O-, -OC(=O)-, -(C=O)NR3, -NR3(C=O)-, -S(O2)NR3-, -NR3S(O2)-, or -NR3(C=O)NR5-, R3 R5 independently hydrogen optionally substituted (C1-C6)alkyl, L1 divalent radical -(Alk1)m(Q)n(Alk2)p- m, n, p, AIk1, AIk2 Q as defined claims; z O 1 ; A represents an mono-, bi- tri-cyclic carbocyclic heterocyclic ring system; -[Linker]- linker radical; R (X) (Y); R1 carboxylic acid group (-COOH), ester which hydrolysable by one more intracellular carboxylesterase enzymes to group; R4 hydrogen; C1-C6 alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 -(C=O)R3, -(C=O)OR3, -(C=O)NR3 heteroary(C1-C6 alkyl)-; R41 alkyl; B monocyclic 5 6 atoms linked carbon adjacent nitrogen shown, fused second case bond shown intersected wavy line may be from atom said ring.
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