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.
