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A new synthesis of spirocyclic oxindole analogue spiro[piperidine-4,3’-pyrrolo[2,3-b]pyridin]-2’(1’H)-one 1 is described.The key steps involve dialkylation of arylacetonitrile and cyclization of the azaoxindole ring by an intramolecular Buchwald-Hartwig amidation of carboxylic ami Je and aryl chloride.A small library was obtained by reductive amination of 1 with various aldehydes and was screened against human lung cancer cell A549,human liver cancer cell BEL7402,and human colon cancer cell HCT-8.The results show that most of the 1(?)rary compounds 2 have some inhibitory activities.2-(Trifluoromethoxy) benzylic substituted spirocyclic azaoxindole 2e was identified as a nanomolar inhibitor against human lung cancer cell A-549(IC_(50)=50 nmol/L).
A new synthesis of spirocyclic oxindole analogue spiro [piperidine-4,3’-pyrrolo [2,3-b] pyridin] -2 ’(1’H) -one 1 is described. The key steps involved in dialkylation of arylacetonitrile and cyclization of the azaoxindole ring by an intramolecular Buchwald-Hartwig amidation of carboxylic ami Je and aryl chloride. A small library was obtained by reductive amination of 1 with various aldehydes and was screened against human lung cancer cell A549, human liver cancer cell BEL 7402, and human colon cancer cell HCT-8.The results show that most of the 1 (?) rary compounds 2 have some inhibitory activities. 2- (Trifluoromethoxy) benzylic substituted spirocyclic azaoxindole 2e was identified as a nanomolar inhibitor against human lung cancer cell A-549 ( IC 50 = 50 nmol / L).