Related Experiment Video
Updated: Apr 22, 2026

Spatiotemporal Subcellular Manipulation of the Microtubule Cytoskeleton in the Living Preimplantation Mouse Embryo using Photostatins
Published on: November 30, 2021
Development of a new benzophenone-diketopiperazine-type potent antimicrotubule agent possessing a 2-pyridine
Yoshiki Hayashi1, Haruka Takeno1, Takumi Chinen2
1Department of Medicinal Chemistry, Tokyo University of Pharmacy and Life Sciences , Hachioji, Tokyo 192-0392, Japan.
Abstract:
A new benzophenone-diketopiperazine-type potent antimicrotubule agent was developed by modifying the structure of the clinical candidate plinabulin (1). Although the right-hand imidazole ring with a branched alkyl chain at the 5-position in 1 was critical for the potency of the antimicrotubule activity, we successfully substituted this moiety with a simpler 2-pyridyl structure by converting the left-hand ring from a phenyl to a benzophenone structure without decreasing the potency. The resultant compound 6b (KPU-300) exhibited a potent cytotoxicity, with an IC50 value of 7.0 nM against HT-29 cells, by strongly binding to tubulin (K d = 1.3 μM) and inducing microtubule depolymerization.
Related Concept Videos
Anthelminthic Agents
Drugs that Stabilize Microtubules
Drugs that Destabilize Microtubules
Destabilization of Microtubules
Antifungal Agents
Microtubule Associated Proteins (MAPs)

