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

Handle URI:
http://hdl.handle.net/10754/562442
Title:
Synthesis of novel 1H-1,2,3-triazole tethered C-5 substituted uracil-isatin conjugates and their cytotoxic evaluation
Authors:
Kumar, Kewal; Sagar, Sunil; Esau, Luke; Kaur, Mandeep; Kumar, Vipan
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 IC50 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. © 2012 Elsevier Masson SAS. All rights reserved.
KAUST Department:
Computational Bioscience Research Center (CBRC); Technology Transfer
Publisher:
Elsevier BV
Journal:
European Journal of Medicinal Chemistry
Issue Date:
Dec-2012
DOI:
10.1016/j.ejmech.2012.10.008
PubMed ID:
23124212
Type:
Article
ISSN:
02235234
Sponsors:
Financial assistance from Department of Science and Technology, New Delhi under Innovation in Science Pursuit for Inspired Research (INSPIRE) Fellowship (KK) is gratefully acknowledged.
Appears in Collections:
Articles; Computational Bioscience Research Center (CBRC)

Full metadata record

DC FieldValue Language
dc.contributor.authorKumar, Kewalen
dc.contributor.authorSagar, Sunilen
dc.contributor.authorEsau, Lukeen
dc.contributor.authorKaur, Mandeepen
dc.contributor.authorKumar, Vipanen
dc.date.accessioned2015-08-03T10:38:20Zen
dc.date.available2015-08-03T10:38:20Zen
dc.date.issued2012-12en
dc.identifier.issn02235234en
dc.identifier.pmid23124212en
dc.identifier.doi10.1016/j.ejmech.2012.10.008en
dc.identifier.urihttp://hdl.handle.net/10754/562442en
dc.description.abstractThe 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 IC50 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. © 2012 Elsevier Masson SAS. All rights reserved.en
dc.description.sponsorshipFinancial assistance from Department of Science and Technology, New Delhi under Innovation in Science Pursuit for Inspired Research (INSPIRE) Fellowship (KK) is gratefully acknowledged.en
dc.publisherElsevier BVen
dc.subject1H-1,2,3-Triazoleen
dc.subjectAnti-cancer evaluationen
dc.subjectClick chemistryen
dc.subjectStructure-activity relationshipen
dc.subjectUracil-isatin conjugatesen
dc.titleSynthesis of novel 1H-1,2,3-triazole tethered C-5 substituted uracil-isatin conjugates and their cytotoxic evaluationen
dc.typeArticleen
dc.contributor.departmentComputational Bioscience Research Center (CBRC)en
dc.contributor.departmentTechnology Transferen
dc.identifier.journalEuropean Journal of Medicinal Chemistryen
dc.contributor.institutionDepartment of Chemistry, Guru Nanak Dev University, Amritsar 143005, Indiaen
kaust.authorSagar, Sunilen
kaust.authorEsau, Lukeen
kaust.authorKaur, Mandeepen

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