作为抗癌剂的 1,3,4-恶二唑:综述。

IF 2.5 4区 医学 Q3 ONCOLOGY
Greesh Kumar, Rajnish Kumar, Avijit Mazumder, Salahuddin, Upendra Kumar
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引用次数: 0

摘要

在最致命的疾病中,癌症的特征是肿瘤或因有丝分裂过程中分裂失控而导致的特定类型细胞数量增加。由于传统的细胞毒性药物具有很大的毒性,当代的研究人员集中精力开发高选择性的抗癌药物。一些已上市的药物分子通过与某些靶点/生长因子/酶(如端粒酶、组蛋白去乙酰化酶(HDAC)、蛋氨酸氨肽酶(MetAP II))相互作用,产生抗癌作用、胸苷酸合成酶(TS)、糖原合成酶激酶-3(GSK)、表皮生长因子(EGF)、血管内皮生长因子(VEGF)、病灶粘附激酶(FAK)、STAT3、胸苷磷酸化酶和碱性磷酸酶。这些药物分子的分子结构中含有各种杂环分子,可发挥药效。最近,1,3,4-噁二唑(五元杂环分子)及其衍生物吸引了研究人员的目光,因为有报道称它们具有广泛的药理活性,包括抗癌活性。1,3,4-噁二唑通过作用于上述任何靶点而显示出抗癌潜力。本研究重点介绍了 1,3,4-噁二唑类抗癌化合物的合成、与靶点的相互作用机制以及与抗癌潜力有关的结构-活性关系。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
1,3,4-Oxadiazoles as Anticancer Agents: A Review.

Among the deadliest diseases, cancer is characterized by tumors or an increased number of a specific type of cell because of uncontrolled divisions during mitosis. Researchers in the current era concentrated on the development of highly selective anticancer medications due to the substantial toxicities of conventional cytotoxic drugs. Several marketed drug molecules have provided resistance against cancer through interaction with certain targets/growth factors/enzymes, such as Telomerase, Histone Deacetylase (HDAC), Methionine Aminopeptidase (MetAP II), Thymidylate Synthase (TS), Glycogen Synthase Kinase-3 (GSK), Epidermal Growth Factor (EGF), Vascular Endothelial Growth Factor (VEGF), Focal Adhesion Kinase (FAK), STAT3, Thymidine phosphorylase, and Alkaline phosphatase. The molecular structure of these drug molecules contains various heterocyclic moieties that act as pharmacophores. Recently, 1,3,4- oxadiazole (five-membered heterocyclic moiety) and its derivatives attracted researchers as these have been reported with a wide range of pharmacological activities, including anti-cancer. 1,3,4- oxadiazoles have exhibited anti-cancer potential via acting on any of the above targets. The presented study highlights the synthesis of anti-cancer 1,3,4-oxadiazoles, their mechanism of interactions with targets, along with structure-activity relationship concerning anti-cancer potential.

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来源期刊
CiteScore
4.50
自引率
7.10%
发文量
55
审稿时长
3 months
期刊介绍: Aims & Scope Recent Patents on Anti-Cancer Drug Discovery publishes review and research articles that reflect or deal with studies in relation to a patent, application of reported patents in a study, discussion of comparison of results regarding application of a given patent, etc., and also guest edited thematic issues on recent patents in the field of anti-cancer drug discovery e.g. on novel bioactive compounds, analogs, targets & predictive biomarkers & drug efficacy biomarkers. The journal also publishes book reviews of eBooks and books on anti-cancer drug discovery. A selection of important and recent patents on anti-cancer drug discovery is also included in the journal. The journal is essential reading for all researchers involved in anti-cancer drug design and discovery. The journal also covers recent research (where patents have been registered) in fast emerging therapeutic areas/targets & therapeutic agents related to anti-cancer drug discovery.
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