| 摘要 |
<p>Cyclopentaquinazoline of formula (I), wherein R1 is hydrogen, amino, C¿1-4? alkyl, C1-4 alkoxy, C1-4 hydroxyalkyl or C1-4 fluoroalkyl; wherein R?2¿ is hydrogen, C¿1-4? alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanoalkyl; Ar?1¿ is phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which may optionally bear one or two substituents selected from halogeno, hydroxy, amino, nitro, cyano, trifluoromethyl, C¿1-4? alkyl and C1-4 alkoxy; and wherein R?3¿ is a group of the formula: -A?1-Ar2-A2-Y1¿, in which A1 is a bond between the α-carbon atom of the group -CONHCH(CO¿2?H)- and Ar?2¿ or is a C¿1-2? alkylene group; Ar?2¿ is phenylene, tetrazoldiyl, tiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which in the case of phenylene may optionally bear one or two substituents on the ring selected from halogeno, nitro, C¿1-4? alkyl and C1-4 alkoxy; A?2¿ is a C¿1-3? alkylene or C2-3 alkenylene group; and a pharmaceutically acceptable salt or ester thereof are of therapeutic value particularly in the treatment of cancer.</p> |
