Related Experiment Video
Updated: May 2, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Developments of kinesin spindle protein inhibitors as antitumor agents based on the five-membered heterocycle
Guo-Dong Zhao, Ren-Zhong Wan, Zhao-Peng Liu1
1Department of Organic Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan 250012, P. R. China. liuzhaop@sdu.edu.cn.
Abstract:
Kinesin spindle protein (KSP) plays an essential role in centrosome separation and formation of the bipolar mitotic spindle. Its exclusive involvement in the mitotic spindle of proliferating cells presents an opportunity for developing new anticancer agents with reduced side effects relative to antimitotics that target tubulin. Small molecule KSP inhibitors have demonstrated their potential as novel antimitotic agents. Several KSP inhibitors have progressed into clinical trials and many others are in preclinical developments. Recently, KSP inhibitors of wide structural diversity have appeared in literatures. This review will summarize the developments of KSP inhibitors based on the five-membered heterocycle scaffolds in recent 10 years. These small molecule KSP inhibitors were classified as dihydropyrazoles, dihydropyrroles, thiophenes, dihydrothiadiazoles, thiazoles and fused pyrroles, their structure-activity relationships were discussed.
More Related Videos
10:33Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
Published on: October 26, 2015
11:49Author Spotlight: Establishing CENP-E Knockout HeLa Cells – A Novel Approach to Study Kinesin-7 CENP-E Biology and its Inhibitors
Published on: June 23, 2023
Related Concept Videos
Inhibition of Cdk Activity
Inhibition of CDK Activity
Drugs that Stabilize Microtubules
Drugs that Destabilize Microtubules
Destabilization of Microtubules
Targeted Cancer Therapies
There are several types of targeted therapies against...