2. Academic Validation
  3. 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

  • Bioorg Med Chem Lett. 2014 Mar 1;24(5):1366-72. doi: 10.1016/j.bmcl.2014.01.044.
Upendar Reddy Chamakura 1,  E Sailaja 2,  Balakrishna Dulla 1,  Arunasree M Kalle 3,  S Bhavani 4,  D Rambabu 5,  Ravikumar Kapavarapu 6,  M V Basaveswara Rao 2,  Manojit Pal 7
Affiliations

Affiliations

  • 1 Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus, Hyderabad 500046, Andhra Pradesh, India.
  • 2 Department of Chemistry, Krishna University, Machilipatnam 521001, Andhra Pradesh, India.
  • 3 Department of Animal Sciences, School of Life Sciences, University of Hyderabad, Gachibowli, Hyderabad 500046, Andhra Pradesh, India.
  • 4 Department of Chemistry, K.L. University, Vaddeswaram, Guntur 522502, Andhra Pradesh, India.
  • 5 Department of Chemistry and the National Institute for Biotechnology in the Negev, Ben-Gurion University of the Negev, Be'er-Sheva 84105, Israel.
  • 6 Doctoral Programme in Experimental Biology and Biomedicine, Center for Neuroscience and Cell Biology, University of Coimbra, 3004-517 Coimbra, Portugal.
  • 7 Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus, Hyderabad 500046, Andhra Pradesh, India. Electronic address: manojitpal@rediffmail.com.
PMID: 24513041 DOI: 10.1016/j.bmcl.2014.01.044
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.

Keywords

Alkyne; Anti-proliferation; Cancer; Coupling; Pd/C.

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