Novel Arylsulfoanilide−Oxindole Hybrid as an Anticancer Agent That Inhibits Translation Initiation

Amarnath Natarajan(Harvard University), Yuhong Guo(Harvard University), Frederick Harbinski(Harvard University), Yun-Hua Fan(Harvard University), Han Chen(Harvard University), Lia Luus(Harvard University), Jana Diercks(Harvard University), Hüseyin Aktaş(Harvard University), Michael Chorev(Harvard University), José A. Halperin(Harvard University)
Journal of Medicinal Chemistry
September 4, 2004
Cited by 186

Abstract

Structure-activity relationship studies of substituted arylsulfoanilides as antiproliferatives, which are mediated by the partial depletion of intracellular Ca(2+) stores, resulted in the identification of compounds with micromolar activity against lung cancer cells in a growth inhibition assay. Incorporating the substitution pattern of the best arylsulfoanilides onto the 3-phenyloxindole scaffold resulted in a potent arylsulfoanilide-oxindole hybrid, 27. Compound 27 inhibits cancer cell growth by partial depletion of intracellular Ca(2+) stores and phosphorylation of eIF2alpha.


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