Synthesis and in vitro anti-proliferative effects of 3-(hetero)aryl substituted 3-[(prop-2-ynyloxy)(thiophen-2-yl)methyl]pyridine derivatives on various cancer cell lines
Synthesis and in vitro anti-proliferative effects of 3-(hetero)aryl substituted 3-[(prop-2-ynyloxy)(thiophen-2-yl)methyl]pyridine derivatives on various cancer cell lines
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Date
2014-03-01
Authors
Reddy Chamakura, Upendar
Sailaja, E.
Dulla, Balakrishna
Kalle, Arunasree M.
Bhavani, S.
Rambabu, D.
Kapavarapu, Ravikumar
Rao, M. V.Basaveswara
Pal, Manojit
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Abstract
A series of 3-(hetero)aryl substituted 3-[(prop-2-ynyloxy)(thiophen-2-yl) methyl]pyridine derivatives were designed as potential anticancer agents. These compounds were conveniently prepared by using Pd/C-Cu mediated Sonogashira type coupling as a key step. Many of these compounds were found to be promising when tested for their in vitro anti-proliferative properties against six cancer cell lines. All these compounds were found to be selective towards the growth inhibition of cancer cells with IC50 values in the range of 0.9-1.7 μM (against MDA-MB 231 and MCF7 cells), comparable to the known anticancer drug doxorubicin. © 2014 Elsevier Ltd. All rights reserved.
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Keywords
Alkyne,
Anti-proliferation,
Cancer,
Coupling,
Pd/C
Citation
Bioorganic and Medicinal Chemistry Letters. v.24(5)