Highlights•Colchicine binding site inhibitors (CBSIs) emerge as new generations of tubulin
inhibitors.•CBSIs are less susceptible to multidrug resistance than FDA-approved tubulin …

It is over 50 years since the discovery of microtubules, and they have become one of the
most important drug targets for anti-cancer therapies. Microtubules are predominantly …

Introduction: About 20 patents have been published from 2013 to 2018 for developing
advanced cancer therapeutics by targeting tubulin polymerization. Currently, there are …

We previously reported a potent tubulin inhibitor CH-2-77. In this study, we optimized the
structure of CH-2-77 by blocking metabolically labile sites and synthesized a series of CH-2 …

Herein, a series of quinazoline and heterocyclic fused pyrimidine analogues were designed
and synthesized based on the X-ray co-crystal structure of lead compound 3a, showing …

Microtubules, formed by α-and β-tubulin heterodimer, are considered as a major target to
prevent the proliferation of tumor cells. Microtubule-targeted agents have become …

Abstract Structurally diverse trimethoxyphenyl-1, 2, 3-triazole hybrids were designed,
synthesized and evaluated for their antiproliferative activity against three cancer cell lines …

The click chemistry is one of the most powerful C− N bond forming‐reactions towards five‐
membered heterocycles. The copper‐catalyzed azide‐alkyne cycloaddition (CuAAC) has …

We recently reported the crystal structure of tubulin in complex with a colchicine binding site
inhibitor (CBSI), ABI-231, having 2-aryl-4-benzoyl-imidazole (ABI). Based on this and …

Due to the three domains of the colchicine-site which is conducive to the combination with
small molecule compounds, colchicine-site on the tubulin has become a common target for …