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  3. Design of new hybrid template by linking quinoline, triazole and dihydroquinoline pharmacophoric groups: A greener approach to novel polyazaheterocycles as cytotoxic agents

Design of new hybrid template by linking quinoline, triazole and dihydroquinoline pharmacophoric groups: A greener approach to novel polyazaheterocycles as cytotoxic agents

  • Bioorg Med Chem Lett. 2015 Mar 1;25(5):1057-63. doi: 10.1016/j.bmcl.2015.01.012.
Koduru Sri Shanthi Praveena 1,  Edupuganti Veera Venkat Shivaji Ramarao 1,  Nandula Yadagiri Sreenivasa Murthy 2,  Surekha Akkenapally 3,  C Ganesh Kumar 3,  Ravikumar Kapavarapu 4,  Sarbani Pal 5
Affiliations

Affiliations

  • 1 MNR Degree & PG College, Kukatpally, Hyderabad 500085, India.
  • 2 Department of Chemistry, School of Engineering, Anurag Group of Institutions, Ranga Reddy District 501301, T.S., India.
  • 3 Chemical Biology Laboratory, Medicinal Chemistry and Pharmacology Division, Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
  • 4 Doctoral Programme in Experimental Biology and Biomedicine, Center for Neuroscience and Cell Biology, University of Coimbra, 3004-517 Coimbra, Portugal.
  • 5 MNR Degree & PG College, Kukatpally, Hyderabad 500085, India. Electronic address: sarbani277@yahoo.com.
PMID: 25655719 DOI: 10.1016/j.bmcl.2015.01.012
Abstract

A new hybrid template designed by linking three pharmacophoric groups, for example, quinoline, triazole and dihydroquinoline moieties have been used for the generation of a library of molecules as potential cytotoxic agents. Synthesis of these polyazaheterocycles were carried out by using a strategy that involved one-pot sequential azidation and CuAAC in water under mild conditions. A number of 1,4-disubstituted 1,2,3-triazoles possessing quinolinylmethylene at N-1 and 1,2-dihydroquinolinyl methylene at C-4 as different substituents were synthesized and evaluated for their cytotoxic effects against various Cancer cells. Some of them showed encouraging activities against lung Cancer cells and one of them showed inhibition of PDE4 indicating the potential medicinal value of these novel polyazaheterocycles.

Keywords

1,2,3-Triazole; Alkyne; Azide; Cancer; PDE4; Quinoline.

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