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

被引：200

作者：

Kaur, Ramandeep ^{[1
]}

Dwivedi, Ashish Ranjan ^{[1
]}

Kumar, Bhupinder ^{[1
]}

Kumar, Vinod ^{[1
]}

机构：

[1] Cent Univ Punjab, Ctr Pharmaceut Sci & Nat Prod, Lab Organ & Med Chem, Bathinda 151001, Punjab, India

来源：

ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY | 2016年 / 16卷 / 04期

关键词：

1,2,4-triazoles; anticancer; kinase inhibitors; tubulin modulators; structure-activity relationship; STEROID SULFATASE INHIBITORS; TUBULIN POLYMERIZATION INHIBITOR; CARBONIC-ANHYDRASE-IX; BIOLOGICAL EVALUATION; IN-VITRO; ANTITUMOR-ACTIVITY; ANTIPROLIFERATIVE ACTIVITY; POTENTIAL ANTITUMOR; AROMATASE INHIBITORS; CELL-DEATH;

D O I：

10.2174/1871520615666150819121106

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

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.

引用

页码：465 / 489

页数：25

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