Kumar Manvendra, Singla Ramit, Dandriyal Jyoti, Jaitak Vikas
Centre for Pharmaceutical Sciences and Natural Products, School of Basic and Applied Sciences, Central University of Punjab, Bathinda, 151 001, India.
Anticancer Agents Med Chem. 2018;18(7):964-984. doi: 10.2174/1871520618666171229185926.
The prevalence of lung cancer is 14% among the newly diagnosed cancer cases worldwide. Currently, the number of drugs that are in clinical practice is having a high prevalence of side effect and multidrug resistance. Researchers have made an attempt to expand a suitable anticancer drug that has no MDR and side effect.
Extensive exploration of Coumarin derivatives as a potent inhibitor of variety of proteins including EGFR, tyrosine kinase, ERK1/2, PI3K, HSP 90, Bax, STAT proteins, NF-κB and telomerase which have been associated with lung cancer.
The recent literature was surveyed utilizing the online resources and databases including scifinder, pubchem, EMBL, scopus and google scholar.
Upon analyzing the structure-activity relationship, it was found that N-aryl carboxamide, phenyl substitution at the C-3 position and 1,2,3- triazolyl, trihydroxystilbene, amino substitution at the C-4 position of the coumarin nucleus were the most effective in targeting lung cancer.
This review is a collaborative and extensive compilation of synthetic strategies, mechanism of action, and the structure-activity relationship thereof for the management of lung carcinoma.
在全球新诊断的癌症病例中，肺癌的患病率为14%。目前，临床实践中使用的药物副作用发生率高且存在多药耐药性。研究人员试图开发一种无多药耐药性和副作用的合适抗癌药物。
广泛探索香豆素衍生物作为多种与肺癌相关蛋白质（包括表皮生长因子受体、酪氨酸激酶、细胞外信号调节激酶1/2、磷脂酰肌醇-3激酶、热休克蛋白90、 Bax蛋白、信号转导和转录激活因子蛋白、核因子κB和端粒酶）的有效抑制剂。
利用包括scifinder、pubchem、欧洲分子生物学实验室、Scopus和谷歌学术在内的在线资源和数据库对近期文献进行调研。
通过分析构效关系发现，N-芳基甲酰胺、香豆素核C-3位的苯基取代以及1,2,3-三唑基、三羟基茋、香豆素核C-4位的氨基取代在靶向肺癌方面最为有效。
本综述是关于肺癌治疗的合成策略、作用机制及其构效关系的综合且广泛的汇编。
