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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

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
24
Issue
5
Identifiers
DOI: 10.1016/j.bmcl.2014.01.044
Keywords
  • Alkyne
  • Coupling
  • Pd/C
  • Cancer
  • Anti-Proliferation
Disciplines
  • Design

Abstract

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 0.9–1.7μM (against MDA-MB 231 and MCF7 cells), comparable to the known anticancer drug doxorubicin.

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