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Abstract
1,2,4-triazole is an important nucleus present in a large number of compounds. More than thirty-five compounds containing this nucleus are introduced into the market. 1,2,4-triazole nucleus is stable to metabolism and acts as an important pharmacophore by interacting at the active site of a receptor as hydrogen bond acceptor and as a donor. Due to its polar nature, the triazole nucleus can increase the solubility of the ligand and it can significantly improve the pharmacological profile of the drug. A large number of 1,2,4-triazole derivatives are reported to possess a wide range of bioactivities including anti-cancer activity. This review article describes the role of 1,2,4-triazole nucleus in different types of anti-cancer agents such as nucleoside based anti-cancer agents, kinase inhibitors, tubulin modulators, aromatase and steroid sulfatase inhibitors, methionine aminopeptidase inhibitors, tankyrase inhibitors and metal complex based anti-cancer agents. It is expected that the current review article will provide insight into various ligand-receptor interactions and help in the rational design and development of novel 1,2,4-triazole based anti-cancer drugs with improved selectivity for cancer cells.
Keywords: 1, 2, 4-triazoles, anticancer, kinase inhibitors, tubulin modulators, structure-activity relationship.
Anti-Cancer Agents in Medicinal Chemistry
Title:Recent Developments on 1,2,4-Triazole Nucleus in Anticancer Compounds: A Review
Volume: 16 Issue: 4
Author(s): Ramandeep Kaur, Ashish Ranjan Dwivedi, Bhupinder Kumar and Vinod Kumar
Affiliation:
Keywords: 1, 2, 4-triazoles, anticancer, kinase inhibitors, tubulin modulators, structure-activity relationship.
Abstract: 1,2,4-triazole is an important nucleus present in a large number of compounds. More than thirty-five compounds containing this nucleus are introduced into the market. 1,2,4-triazole nucleus is stable to metabolism and acts as an important pharmacophore by interacting at the active site of a receptor as hydrogen bond acceptor and as a donor. Due to its polar nature, the triazole nucleus can increase the solubility of the ligand and it can significantly improve the pharmacological profile of the drug. A large number of 1,2,4-triazole derivatives are reported to possess a wide range of bioactivities including anti-cancer activity. This review article describes the role of 1,2,4-triazole nucleus in different types of anti-cancer agents such as nucleoside based anti-cancer agents, kinase inhibitors, tubulin modulators, aromatase and steroid sulfatase inhibitors, methionine aminopeptidase inhibitors, tankyrase inhibitors and metal complex based anti-cancer agents. It is expected that the current review article will provide insight into various ligand-receptor interactions and help in the rational design and development of novel 1,2,4-triazole based anti-cancer drugs with improved selectivity for cancer cells.
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Cite this article as:
Kaur Ramandeep, Dwivedi Ranjan Ashish, Kumar Bhupinder and Kumar Vinod, Recent Developments on 1,2,4-Triazole Nucleus in Anticancer Compounds: A Review, Anti-Cancer Agents in Medicinal Chemistry 2016; 16 (4) . https://dx.doi.org/10.2174/1871520615666150819121106
DOI https://dx.doi.org/10.2174/1871520615666150819121106 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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