Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Cu-mediated synthesis of 2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-1-ones as potential inhibitors of sirtuins

Author(s): Sreerama Srinivas Rao, Dandela Rambabu, Mohosin Layek, Kummari Lalith Kumar, Mandava Venkata Basaveswara Rao, Devyani Haldar, Manojit Pal.

Abstract:

CuI facilitated the intramolecular cyclization of 8-alkynyl substituted 2,3-dihydroquinolin-4(1H)-ones leading to 5-subtituted 2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-1-ones via intramolecular C-N bond forming reaction. Some of the synthesized compounds have shown encouraging inhibition of Sir 2 protein (a yeast homolog of mammalian SIRT1) when tested using a yeast cell based assay. A representative compound showed dose dependent inhibition of yeast Sir 2 (IC50 = 30.09 µM) and cell growth inhibition properties when tested against different cancer cell lines. It’s in silico interactions with sirtuins are presented.

Keywords: Alkyne, CuI, Cyclization, Docking, Pyrroloquinolines, Sirtuins.

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Article Details

VOLUME: 11
ISSUE: 2
Year: 2014
Page: [199 - 206]
Pages: 8
DOI: 10.2174/15701808113109990065
Price: $58