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

Year: 2016
Type: article
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.
DOI: 10.1021/acs.jmedchem.6b00400
Authors: Sandeep Rana, Elizabeth C. Blowers, Calvin Tebbe, Jacob I. Contreras, Prakash Radhakrishnan, Smitha Kizhake, Tian Zhou, Rajkumar N. Rajule, Jamie L. Arnst, Adnan R. Munkarah, Ramandeep Rattan, Amarnath Natarajan
Language: English
Field: Chemistry
Open Access status: green
Awards: G269183255, G2957411659, G3373492060, G5511633969, Buffett Cancer Center Support Grant, Cancer Biology Training Program, G911360726
OpenAlex ID: W2336869895
FWCI: 4.902
Cites: 46
Cited by: 112
Related to: 10