Cu-mediated synthesis of 2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-1-ones as potential inhibitors of sirtuins
Sreerama Srinivas Rao,
Kummari Lalith Kumar,
Mandava Venkata Basaveswara Rao,
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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