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  • Title: 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.
    Author: Reddy Chamakura U, Sailaja E, Dulla B, Kalle AM, Bhavani S, Rambabu D, Kapavarapu R, Rao MV, Pal M.
    Journal: Bioorg Med Chem Lett; 2014 Mar 01; 24(5):1366-72. PubMed ID: 24513041.
    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.
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