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Heterocycles - Synthesis and Biological Activities最新文献

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Thiazole Moiety: An Interesting Scaffold for Developing New Antitumoral Compounds 噻唑基团:开发新的抗肿瘤化合物的一个有趣的支架
Pub Date : 2019-01-17 DOI: 10.5772/INTECHOPEN.82741
Sandra Ramos-Inza, Carlos Aydillo, C. Sanmartín, D. Plano
Currently, cancer is one of the major health problems of the human population and prominent cause of death. Thiazole ring has demonstrated many pharmacological activities including anticancer. This scaffold has been found alone or incorporated into the diversity of therapeutic active agents such as tiazofurin, dasatinib, and bleomycin, which are well-known antineoplastic drugs. Recently, most of the compounds isolated from natural sources containing thiazole moiety exhibit notable cytotoxicities and present antitumor potential. In this context, several structural changes have been made in the original structure, such as the incorporation of different substituents or the fusion with other carbo- and heterocycles, in order to increase the antitumoral potency. Related to mechanism of action of these derivatives, some of them act through kinase modulation, polymerization inhibition of microtubule, pro-matrix metalloproteinase activation, signal transducer activation of transcription 3, histone deacetylase inhibition, etc.
目前,癌症是人类的主要健康问题之一,也是人类死亡的主要原因之一。噻唑环具有多种药理活性,包括抗癌作用。这种支架已被发现单独或合并到多种治疗活性药物中,如噻唑呋喃、达沙替尼和博来霉素,这些都是众所周知的抗肿瘤药物。近年来,从天然来源分离的含有噻唑基团的化合物大多具有显著的细胞毒性和抗肿瘤潜力。在这种情况下,为了增加抗肿瘤效力,在原始结构上进行了一些结构改变,例如加入不同的取代基或与其他碳环和杂环融合。这些衍生物的作用机制包括激酶调节、微管聚合抑制、前基质金属蛋白酶激活、转录3信号转导激活、组蛋白去乙酰化酶抑制等。
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引用次数: 16
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Heterocycles - Synthesis and Biological Activities
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