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ID: ALA3822425

Journal: J Med Chem

Title: Isatin Derived Spirocyclic Analogues with α-Methylene-γ-butyrolactone as Anticancer Agents: A Structure-Activity Relationship Study.

Authors: Rana S, Blowers EC, Tebbe C, Contreras JI, Radhakrishnan P, Kizhake S, Zhou T, Rajule RN, Arnst JL, Munkarah AR, Rattan R, Natarajan A.

Abstract: Design, synthesis, and evaluation of α-methylene-γ-butyrolactone analogues and their evaluation as anticancer agents is described. SAR identified a spirocyclic analogue 19 that inhibited TNFα-induced NF-κB activity, cancer cell growth and tumor growth in an ovarian cancer model. A second iteration of synthesis and screening identified 29 which inhibited cancer cell growth with low-μM potency. Our data suggest that an isatin-derived spirocyclic α-methylene-γ-butyrolactone is a suitable core for optimization to identify novel anticancer agents.

CiteXplore: 27077228

DOI: 10.1021/acs.jmedchem.6b00400