Natural Product-Derived Spirooxindole Fragments Serve as Privileged Substructures for Discovery of New Anticancer Agents

Author(s): Bin Yu, Yi-Chao Zheng, Xiao-Jing Shi, Ping-Ping Qi, Hong-Min Liu

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 16 , Issue 10 , 2016

Become EABM
Become Reviewer
Call for Editor

Graphical Abstract:


The utility of natural products for identifying anticancer agents has been highly pursued in the last decades and over 100 drug molecules in clinic are natural products or natural product-derived compounds. Natural products are believed to be able to cover unexplored chemical space that is normally not occupied by commercially available molecule libraries. However, the low abundance and synthetic intractability of natural products have limited their applications in drug discovery. Recently, the identification of biologically relevant fragments derived from biologically validated natural products has been recognized as a powerful strategy in searching new biological probes and drugs. The spirocyclic oxindoles, as privileged structural scaffolds, have shown their potential in designing new drugs. Several anticancer drug candidates such as SAR405838, RO8994, CFI-400945 and their bioisosteres are undergoing clinical trials or preclinical studies. To highlight the significant progress, we focus on illustrating the discovery of SAR405838, RO8994, CFI-400945 and their bioisosteres for cancer therapy using substructure-based strategies and discussing modes of action, binding models and preclinical data.

Keywords: Anticancer agents, cancer therapy, MDM2 inhibitors, natural products, PLK4 inhibitors, spirooxindoles.

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2016
Page: [1315 - 1324]
Pages: 10
DOI: 10.2174/1871520615666151102093825
Price: $65

Article Metrics

PDF: 71
PRC: 1