Structure-activity relationship (SAR) study and design strategies of nitrogen-containing heterocyclic moieties for their anticancer activities

被引：434
作者：
Akhtar, Jawaid [1 ]
Khan, Ahsan Ahmed [1 ]
Ali, Zulphikar [1 ]
Haider, Rafi [1 ]
Yar, M. Shahar [1 ]
机构：
[1] Hamdard Univ, Dept Pharmaceut Chem, Fac Pharm, New Delhi 110062, India
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2017年 / 125卷
关键词：
Anticancer; Cytotoxic; SARs; N-Heterocycles; HISTONE DEACETYLASE INHIBITORS; ANTITUMOR-ACTIVITY EVALUATION; HIGHLY SELECTIVE LIGANDS; IN-VITRO EVALUATION; BIOLOGICAL EVALUATION; ANTIPROLIFERATIVE ACTIVITY; POTENTIAL ANTITUMOR; AGENTS DESIGN; DNA-BINDING; PHARMACOLOGICAL EVALUATION;
D O I：
10.1016/j.ejmech.2016.09.023
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The present review article offers a detailed account of the design strategies employed for the synthesis of nitrogen-containing anticancer agents. The results of different studies describe the N-heterocyclic ring system is a core structure in many synthetic compounds exhibiting a broad range of biological activities. Benzimidazole, benzothiazole, indole, acridine, oxadiazole, imidazole, isoxazole, pyrazole, triazoles, quinolines and quinazolines including others drugs containing pyridazine, pyridine and pyrimidines are covered. The following studies of these compounds suggested that these compounds showed their antitumor activities through multiple mechanisms including inhibiting protein kinase (CDK, MK-2, PLK1, kinesin-like protein Eg5 and IKK), topoisomerase I and II, microtubule inhibition, and many others. Our concise representation exploits the design and anticancer potency of these compounds. The direct comparison of anticancer activities with the standard enables a systematic analysis of the structure activity relationship among the series. (C) 2016 Elsevier Masson SAS. All rights reserved.
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收藏
页码：143 / 189
页数：47
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