1. Academic Validation
  2. The importance of indole and azaindole scaffold in the development of antitumor agents

The importance of indole and azaindole scaffold in the development of antitumor agents

  • Eur J Med Chem. 2020 Oct 1:203:112506. doi: 10.1016/j.ejmech.2020.112506.
Yu Han 1 Wei Dong 1 Qunqun Guo 2 Xiufen Li 1 Longjiang Huang 3
Affiliations

Affiliations

  • 1 State Key Laboratory Base for Eco-Chemical Engineering, College of Chemical Engineering, Qingdao University of Science and Technology, 53 Zhengzhou Road, Qingdao, 266042, China.
  • 2 College of Life Sciences, Qingdao University, Qingdao, China.
  • 3 State Key Laboratory Base for Eco-Chemical Engineering, College of Chemical Engineering, Qingdao University of Science and Technology, 53 Zhengzhou Road, Qingdao, 266042, China; State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 1 Xiannongtan Street, Xicheng District, Beijing, 100050, China. Electronic address: huanglj@qust.edu.cn.
Abstract

With some indoles and azaindoles being successfully developed as Anticancer drugs, the design and synthesis of indole and azaindole derivatives with remarkable antitumor activity has received increasing attention and significant progress has been made. This paper reviews the recent progress in the study of tumorigenesis, mechanism of actions and structure activity relationships about Anticancer indole and azindole derivatives. Combining structure activity relationships and molecular targets-related knowledge, this review will help researchers design more effective, safe and cost-effective Anticancer indoles and azindoles agents.

Keywords

Antiproliferative activity; Antitumor activity; Azaindole derivatives; Cytotoxicity; Indole derivatives.

Figures