2. Academic Validation
  3. Aplysinopsin analogs: Synthesis and anti-proliferative activity of substituted (Z)-5-(N-benzylindol-3-ylmethylene)imidazolidine-2,4-diones

Aplysinopsin analogs: Synthesis and anti-proliferative activity of substituted (Z)-5-(N-benzylindol-3-ylmethylene)imidazolidine-2,4-diones

  • Bioorg Med Chem. 2010 May 15;18(10):3570-4. doi: 10.1016/j.bmc.2010.03.054.
Y Thirupathi Reddy 1,  P Narsimha Reddy,  Srinivas Koduru,  Chendil Damodaran,  Peter A Crooks
Affiliations

Affiliation

  • 1 Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536, USA.
PMID: 20403701 DOI: 10.1016/j.bmc.2010.03.054
Abstract

A series of substituted (Z)-5-(N-benzylindol-3-ylmethylene)imidazolidine-2,4-dione (3) analogs structurally related to aplysinopsin, and that incorporate a variety of substituents in both the indole and N-benzyl moieties have been synthesized under microwave irradiation and conventional heating methods These analogs were evaluated for their anti-proliferative activity against MCF-7 and MDA-231 breast Cancer cell lines, and A549 and H460 lung Cancer cell lines. Two analogs, 3f and 3j had IC(50) values of 4.4 and 5.2microM, respectively, compared to 5-fluorouracil (IC(50)=15.2microM) against MCF-7 cells.

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