Literature DB >> 27077228

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

Sandeep Rana, Elizabeth C Blowers, Calvin Tebbe1, Jacob I Contreras, Prakash Radhakrishnan, Smitha Kizhake, Tian Zhou, Rajkumar N Rajule, Jamie L Arnst, Adnan R Munkarah1, Ramandeep Rattan1, Amarnath Natarajan.   

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.

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Year:  2016        PMID： 27077228      PMCID： PMC5273401          DOI： 10.1021/acs.jmedchem.6b00400

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  44 in total

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10.  Structure activity relationship (SAR) study identifies a quinoxaline urea analog that modulates IKKβ phosphorylation for pancreatic cancer therapy.

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