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

Kewal Kumar; Sunil Sagar; Luke Esau; Mandeep Kaur; Vipan Kumar

doi:10.1016/j.ejmech.2012.10.008

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

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

Computer, Electrical and Mathematical Sciences and Engineering

Research output: Contribution to journal › Article › peer-review

65 Scopus citations

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.

Original language	English (US)
Pages (from-to)	153-159
Number of pages	7
Journal	European Journal of Medicinal Chemistry
Volume	58
DOIs	https://doi.org/10.1016/j.ejmech.2012.10.008
State	Published - Dec 2012

Bibliographical note

KAUST Repository Item: Exported on 2020-10-01
Acknowledgements: Financial assistance from Department of Science and Technology, New Delhi under Innovation in Science Pursuit for Inspired Research (INSPIRE) Fellowship (KK) is gratefully acknowledged.

ASJC Scopus subject areas

Organic Chemistry
Drug Discovery
Pharmacology

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This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.ejmech.2012.10.008

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

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. {\textcopyright} 2012 Elsevier Masson SAS. All rights reserved.",

author = "Kewal Kumar and Sunil Sagar and Luke Esau and Mandeep Kaur and Vipan Kumar",

note = "KAUST Repository Item: Exported on 2020-10-01 Acknowledgements: Financial assistance from Department of Science and Technology, New Delhi under Innovation in Science Pursuit for Inspired Research (INSPIRE) Fellowship (KK) is gratefully acknowledged.",

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AU - Kumar, Kewal

AU - Sagar, Sunil

AU - Esau, Luke

AU - Kaur, Mandeep

AU - Kumar, Vipan

N1 - KAUST Repository Item: Exported on 2020-10-01 Acknowledgements: Financial assistance from Department of Science and Technology, New Delhi under Innovation in Science Pursuit for Inspired Research (INSPIRE) Fellowship (KK) is gratefully acknowledged.

PY - 2012/12

Y1 - 2012/12

N2 - 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.

AB - 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.

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DO - 10.1016/j.ejmech.2012.10.008

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SN - 0223-5234

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SP - 153

EP - 159

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

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

Abstract

Bibliographical note

ASJC Scopus subject areas

UN SDGs

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