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Role of Indole Scaffolds as Pharmacophores in the Development of Anti-Lung Cancer Agents
Molecules ( IF 4.6 ) Pub Date : 2020-04-01 , DOI: 10.3390/molecules25071615
Jyothi Dhuguru 1 , Rachid Skouta 1
Affiliation  

Lung cancer is the leading cause of death in men and women worldwide, affecting millions of people. Between the two types of lung cancers, non-small cell lung cancer (NSCLC) is more common than small cell lung cancer (SCLC). Besides surgery and radiotherapy, chemotherapy is the most important method of treatment for lung cancer. Indole scaffold is considered one of the most privileged scaffolds in heterocyclic chemistry. Indole may serve as an effective probe for the development of new drug candidates against challenging diseases, including lung cancer. In this review, we will focus on discussing the existing indole based pharmacophores in the clinical and pre-clinical stages of development against lung cancer, along with the synthesis of some of the selected anti-lung cancer drugs. Moreover, the basic mechanism of action underlying indole based anti-lung cancer treatment, such as protein kinase inhibition, histone deacetylase inhibition, DNA topoisomerase inhibition, and tubulin inhibition will also be discussed.

中文翻译:

吲哚支架作为药效团在抗肺癌药物开发中的作用

肺癌是全世界男性和女性死亡的主要原因,影响了数百万人。在两种肺癌中,非小细胞肺癌(NSCLC)比小细胞肺癌(SCLC)更常见。除了手术和放疗,化疗是肺癌最重要的治疗方法。吲哚支架被认为是杂环化学中最有特权的支架之一。吲哚可作为一种有效的探针,用于开发针对具有挑战性的疾病(包括肺癌)的新候选药物。在这篇综述中,我们将重点讨论在肺癌的临床和临床前开发阶段中现有的基于吲哚的药效团,以及一些选定的抗肺癌药物的合成。而且,
更新日期:2020-04-01
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