Literature DB >> 23124212

Synthesis of novel 1H-1,2,3-triazole tethered C-5 substituted uracil-isatin conjugates and their cytotoxic evaluation.

Kewal Kumar1, Sunil Sagar, Luke Esau, Mandeep Kaur, Vipan Kumar.   

Abstract

The present manuscript describes the synthesis of uracil-isatin hybrids via azide-alkyne cycloadditions and their cytotoxic evaluation against three human cancer cell lines viz. HeLa (cervix), MCF-7 (breast) and DU145 (prostate) using MTT assay. The evaluation studies revealed the dependence of cytotoxicity on C-5 substituents of both uracil and isatin as well as the alkyl chain length with compounds 6g and 6k showing IC(50) values 18.21 and 13.90 μM respectively against DU145 cell lines. Most of the synthesized conjugates exhibited considerable selectivity against MCF-7 and DU145 cell lines.
Copyright © 2012 Elsevier Masson SAS. All rights reserved.

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Year:  2012        PMID: 23124212     DOI: 10.1016/j.ejmech.2012.10.008

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  4 in total

Review 1.  Rational approaches, design strategies, structure activity relationship and mechanistic insights for therapeutic coumarin hybrids.

Authors:  Harbinder Singh; Jatinder Vir Singh; Kavita Bhagat; Harmandeep Kaur Gulati; Mohit Sanduja; Nitish Kumar; Nihar Kinarivala; Sahil Sharma
Journal:  Bioorg Med Chem       Date:  2019-06-22       Impact factor: 3.641

2.  A green, multicomponent, regio- and stereo-selective 1,3-dipolar cycloaddition of azides and azomethine ylides generated in situ with bifunctional dipolarophiles using PEG-400.

Authors:  Jayant Sindhu; Harjinder Singh; J M Khurana
Journal:  Mol Divers       Date:  2014-02-28       Impact factor: 2.943

3.  1H-1,2,3-triazole tethered isatin-ferrocene conjugates: Synthesis and in vitro antimalarial evaluation.

Authors:  Kewal Kumar; Bruno Pradines; Marilyn Madamet; Rémy Amalvict; Nicolas Benoit; Vipan Kumar
Journal:  Eur J Med Chem       Date:  2014-10-13       Impact factor: 6.514

4.  N-Propargylated isatin-Mannich mono- and bis-adducts: synthesis and preliminary analysis of in vitro activity against Tritrichomonas foetus.

Authors:  Kewal Kumar; Gaurav Bhargava; Kirkwood M Land; Kai-Hsiang Chang; Reena Arora; Somdutta Sen; Vipan Kumar
Journal:  Eur J Med Chem       Date:  2014-01-18       Impact factor: 6.514

  4 in total

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