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

作者：Praveena Koduru Sri Shanthi; Ramarao Edupuganti Veera Venkat Shivaji; Murthy Nandula Yadagiri Sreenivasa; Akkenapally Surekha; Kumar C Ganesh; Kapavarapu Ravikumar; Pal Sarbani^*

来源：Bioorganic & Medicinal Chemistry Letters, 2015, 25(5): 1057-1063.

DOI：10.1016/j.bmcl.2015.01.012

• Quinoline
• 1,2,3-Triazole
• Azide
• Alkyne
• Cancer
• PDE4

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.

• 出版日期2015-3-1