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 …

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 …

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 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 …

Scaffold-retained structure generator to exhaustively create molecules in an arbitrary chemical space

K Kaitoh, Y Yamanishi - Journal of Chemical Information and …, 2022 - ACS Publications
The construction of a virtual library (VL) consisting of novel molecules based on structure–
activity relationships is crucial for lead optimization in rational drug design. In this study, we …

Design, synthesis and evaluation of 4-phenyl-1, 2, 3-triazole substituted pyrimidine derivatives as antiproliferative and tubulin polymerization inhibitors

AR Dwivedi, V Kumar, RP Yadav, N Kumar… - Journal of Molecular …, 2022 - Elsevier
Ligands binding to the colchicine domain of the tubulin protein act as tubulin polymerization
inhibitors and arrest the cell cycle in G2/M phase. A series of 4-Phenyl-1, 2, 3-triazole …

Discovery of novel tubulin inhibitors targeting the colchicine binding site via virtual screening, structural optimization and antitumor evaluation

W Liu, H Jia, M Guan, M Cui, Z Lan, Y He, Z Guo… - Bioorganic …, 2022 - Elsevier
The colchicine binding site of tubulin is a promising target for discovering novel antitumor
agents which exert the antiangiogenic effect and are not susceptible to multidrug resistance …

Design, synthesis and biological investigation of 2-anilino triazolopyrimidines as tubulin polymerization inhibitors with anticancer activities

R Romagnoli, P Oliva, F Prencipe, S Manfredini… - Pharmaceuticals, 2022 - mdpi.com
A further investigation aiming to generate new potential antitumor agents led us to
synthesize a new series of twenty-two compounds characterized by the presence of the 7 …

Colchicine-binding site agent CH-2-77 as a potent tubulin inhibitor suppressing triple-negative breast cancer

S Deng, RI Krutilina, KL Hartman, H Chen… - Molecular cancer …, 2022 - AACR
Triple-negative breast cancer (TNBC) is a highly aggressive type of breast cancer. Unlike
other subtypes of breast cancer, TNBC lacks hormone and growth factor receptor targets …