Recent Developments on 1,2,4-Triazole Nucleus in Anticancer Compounds: A Review

Author(s): Ramandeep Kaur, Ashish Ranjan Dwivedi, Bhupinder Kumar, Vinod Kumar

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 16 , Issue 4 , 2016

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Graphical 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.

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Article Details

Year: 2016
Published on: 18 February, 2016
Page: [465 - 489]
Pages: 25
DOI: 10.2174/1871520615666150819121106
Price: $65

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