| abstract |
Compounds of formula (I) have HSP90 inhibitory activity: n n n n n n n n n n ring A is an aryl or heteroaryl ring or ring system; R 1 is hydrogen, fluoro, chloro, bromo, or a radical of formula (1A): —X-Alk 1 -(Z) m -(Alk 2 ) n -Q (IA) wherein X is a bond, —O—, —S—, —S(O)—, —SO 2 —, or —NH—, Z is —O—, —S—, —(C═O)—, —(C═S)—, —S(O)—, —SO 2 —, —NR A —, or, in either orientation —C(═O)O—, —C(═O)NR A —, —C(═S)NR A —, —SO 2 NR A —, —NR A C(═O)—, or —NR A SO 2 — wherein R A is hydrogen or C 1 -C 6 alkyl in which one or more hydrogens is optionally substituted by fluorine; Alk 1 and Alk 2 are optionally substituted divalent C 1 -C 3 alkylene or C 2 -C 3 alkenylene radicals, m and n are independently 0 or 1, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R 2 is cyano (—CN), fluoro, chloro, bromo, methyl, ethyl, —OH, —CH 2 OH, —C(═O)NH 2 , —C(═O)H, —C(═O)CH 3 , or —NH 2 ; R 3 and R 4 are independently selected from hydrogen, fluoro, chloro, bromo, cyano (—CN), C 1 -C 3 alkyl optionally substituted with one or more fluorine substituents, C 1 -C 3 alkoxy optionally substituted with one or more fluorine substituents, —CH═CH 2 , —C≡CH, cyclopropyl and —NH 2 , or R 3 and R 4 together represent methylenedioxy (—OCH 2 O—) or ethylenedioxy (—OCH 2 CH 2 O—) in either of which one or more hydrogens are optionally replaced by fluorine; S 1 is as defined in the description. |