| abstract |
The present invention provides novel indole derivatives of formula (I): (I) wherein R1 is lower alkyl, lower alkenyl, (hydroxy)lower alkyl, lower alkynyl, phenyl, benzyl or 2-thienyl, R?2, R3, R4 and R5¿ are the same or different and are each hydrogen or lower alkyl; each R6 is individually hydrogen, lower alkyl, hydroxy, (hydroxy)lower alkyl, lower alkoxy, benzyloxy, lower alkanoyloxy, nitro or halo, n is 1-3, R7 is hydrogen, lower alkyl or lower alkenyl, X is oxy and thio, Y is carbonyl, (CH¿2?)1-3,(CH2)1-3SO2 or (CH2)1-3C(O), and Z is (φ-(4-pyridyl)(C2-C4 alkoxy), (φ-((R?8)(R9¿) amino)(C¿2?-C4 alkoxy), wherein R?8 and R9¿ are each H, (C¿1?-C3)alkyl or together with N are a 5- or 6-membered heterocyclic ring comprising 1-3 N(R?8¿), S or nonperoxide O; an amino acid ester of (φ-(HO)(C¿2?-C4))alkoxy, N(R?8)CH(R8)CO¿2H, 1'-D-glucuronyloxy; or Y-Z is (CH2)1-3R8; wherein R8 is OH, (C¿2?-C4)acyloxy, SO3H, PO4H2, N(NO)(OH), SO2NH2, PO(OH)(NH2), or a tetrazolyl; or a pharmaceutically acceptable salt thereof, useful to inhibit cancer or sensitize cancer cells to chemotherapeutic agents, radiation or other anti-cancer treatments. |