Recent advances of tubulin inhibitors targeting the colchicine binding site for cancer therapy

M Hawash - Biomolecules, 2022 - mdpi.com
Cancer accounts for numerous deaths each year, and it is one of the most common causes
of death worldwide, despite many breakthroughs in the discovery of novel anticancer …

An update on the recent advances and discovery of novel tubulin colchicine binding inhibitors

H Weng, J Li, H Zhu, KF Carver Wong… - Future Medicinal …, 2023 - Taylor & Francis
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 …

Discovery of novel coumarin-indole derivatives as tubulin polymerization inhibitors with potent anti-gastric cancer activities

J Song, YF Guan, WB Liu, CH Song, XY Tian… - European Journal of …, 2022 - Elsevier
Novel coumarin-indole derivatives were designed, synthesized and evaluated as tubulin
polymerization inhibitors targeting the colchicine binding site. Among these compounds …

Discovery of novel acridane-based tubulin polymerization inhibitors with anticancer and potential immunomodulatory effects

X Peng, Y Ren, W Pan, J Liu… - Journal of medicinal …, 2022 - ACS Publications
A series of novel acridane-based tubulin polymerization inhibitors were designed,
synthesized, and bioevaluated as anticancer agents. The most potent compound NT-6 …

Synthesis and biological evaluation of structurally diverse 6-aryl-3-aroyl-indole analogues as inhibitors of tubulin polymerization

W Ren, Y Deng, JD Ward, R Vairin, R Bai… - European Journal of …, 2024 - Elsevier
The synthesis and evaluation of small-molecule inhibitors of tubulin polymerization remains
a promising approach for the development of new therapeutic agents for cancer treatment …

SB226, an inhibitor of tubulin polymerization, inhibits paclitaxel-resistant melanoma growth and spontaneous metastasis

S Deng, S Banerjee, H Chen, S Pochampally, Y Wang… - Cancer letters, 2023 - Elsevier
Extensive preclinical studies have shown that colchicine-binding site inhibitors (CBSIs) are
promising drug candidates for cancer therapy. Although numerous CBSIs were generated …

Sabizabulin, a potent orally bioavailable colchicine binding site agent, suppresses HER2+ breast cancer and metastasis

RI Krutilina, KL Hartman, D Oluwalana, HC Playa… - Cancers, 2022 - mdpi.com
Simple Summary The sabizabulin agent represses tumor cell growth, cell migration, and
colony formation, and induces cell death in HER2+ breast cancer models. Sabizabulin is …

Design, synthesis, and biological evaluation of pyrimidine dihydroquinoxalinone derivatives as tubulin colchicine site-binding agents that displayed potent anticancer …

S Pochampally, KL Hartman, R Wang… - ACS Pharmacology & …, 2023 - ACS Publications
Polymerization of tubulin dimers to form microtubules is one of the key events in cell
proliferation. The inhibition of this event has long been recognized as a potential treatment …

Insights into the Pharmacological Activity of the Imidazo− Pyrazole Scaffold

A Spallarossa, F Rapetti, MG Signorello… - …, 2023 - Wiley Online Library
In previous studies, we synthesized different imidazo− pyrazoles 1 and 2 with interesting
anticancer, anti‐angiogenic and anti‐inflammatory activities. To further extend the structure …

Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site

XY Yan, JF Leng, TT Chen, YJ Zhao, LY Kong… - European Journal of …, 2022 - Elsevier
A novel series of diphenylamine derivatives were designed and synthesized, and their
biological activities were evaluated. The anti-proliferative activities of the derivatives were …