Literature DB >> 25655719

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

Koduru Sri Shanthi Praveena1, Edupuganti Veera Venkat Shivaji Ramarao1, Nandula Yadagiri Sreenivasa Murthy2, Surekha Akkenapally3, C Ganesh Kumar3, Ravikumar Kapavarapu4, Sarbani Pal5.   

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.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

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

Mesh:

Substances:

Year:  2015        PMID: 25655719     DOI: 10.1016/j.bmcl.2015.01.012

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

Review 1.  Tailored Quinolines Demonstrate Flexibility to Exert Antitumor Effects through Varied Mechanisms-A Medicinal Perspective.

Authors:  Sachin Sharma; Arshdeep Singh; Sahil Sharma; Ram Sharma; Jagjeet Singh; Nihar Kinarivala; Kunal Nepali; Jing P Liou
Journal:  Anticancer Agents Med Chem       Date:  2021       Impact factor: 2.527

2.  Amidine- and Amidoxime-Substituted Heterocycles: Synthesis, Antiproliferative Evaluations and DNA Binding.

Authors:  Silvija Maračić; Petra Grbčić; Suresh Shammugam; Marijana Radić Stojković; Krešimir Pavelić; Mirela Sedić; Sandra Kraljević Pavelić; Silvana Raić-Malić
Journal:  Molecules       Date:  2021-11-22       Impact factor: 4.411

3.  Monitoring glycosidase activity for clustered sugar substrates, a study on β-glucuronidase.

Authors:  Yoan Brissonnet; Guillaume Compain; Brigitte Renoux; Eva-Maria Krammer; Franck Daligault; David Deniaud; Sébastien Papot; Sébastien G Gouin
Journal:  RSC Adv       Date:  2019-12-04       Impact factor: 4.036

Review 4.  CuAAC-ensembled 1,2,3-triazole-linked isosteres as pharmacophores in drug discovery: review.

Authors:  Alisha Rani; Gurjaspreet Singh; Akshpreet Singh; Ubair Maqbool; Gurpreet Kaur; Jandeep Singh
Journal:  RSC Adv       Date:  2020-02-04       Impact factor: 4.036

5.  Microwave-assisted synthesis, biological evaluation and molecular docking studies of new coumarin-based 1,2,3-triazoles.

Authors:  Ravinder Dharavath; Nalaparaju Nagaraju; M Ram Reddy; D Ashok; M Sarasija; M Vijjulatha; Vani T; K Jyothi; G Prashanthi
Journal:  RSC Adv       Date:  2020-03-23       Impact factor: 4.036

6.  Synthesis and In Vitro Cytotoxicity and Antibacterial Activity of Novel 1,2,3-Triazol-5-yl-phosphonates.

Authors:  Anna Tripolszky; Emese Tóth; Pál Tamás Szabó; László Hackler; Beáta Kari; László G Puskás; Erika Bálint
Journal:  Molecules       Date:  2020-06-06       Impact factor: 4.411

  6 in total

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