Department of Biology, University of Massachusetts, Amherst, MA 01003, USA.
Molecules. 2020 Apr 1;25(7):1615. doi: 10.3390/molecules25071615.
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.
肺癌是全球男性和女性的主要死亡原因，影响了数百万人。在两种类型的肺癌中，非小细胞肺癌（NSCLC）比小细胞肺癌（SCLC）更为常见。除了手术和放疗外，化疗是治疗肺癌最重要的方法。吲哚骨架被认为是杂环化学中最具特权的骨架之一。吲哚可以作为开发针对包括肺癌在内的挑战性疾病的新药候选物的有效探针。在这篇综述中，我们将重点讨论现有的临床和临床前阶段针对肺癌的基于吲哚的药效团，以及一些选定的抗癌药物的合成。此外，还将讨论基于吲哚的抗癌治疗的基本作用机制，如蛋白激酶抑制、组蛋白去乙酰化酶抑制、DNA 拓扑异构酶抑制和微管蛋白抑制。
