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 …

A Metal-Free strategy for the synthesis of tetrasubstituted Pyridines: Dimethyl sulfoxide as carbon source

XY Zhang, K Liu, S Li, Y Li, Y Wu, X Li, X Ran, A Liu… - Tetrahedron …, 2023 - Elsevier
An efficient and practical approach for the synthesis of tetrasubstituted pyridines has been
described via the Imidazole hydrochloride-promoted reaction of enaminones with DMSO …

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 …

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 …

Structure-Based Optimization of Carbendazim-Derived Tubulin Polymerization Inhibitors through Alchemical Free Energy Calculations

L Cano-González, JD Espinosa-Mendoza… - Journal of Chemical …, 2023 - ACS Publications
Carbendazim derivatives, commonly used as antiparasitic drugs, have shown potential as
anticancer agents due to their ability to induce cell cycle arrest and apoptosis in human …

Discovery of potent tubulin inhibitors targeting the colchicine binding site via structure-based lead optimization and antitumor evaluation

W Liu, Y He, Z Guo, M Wang, X Han, H Jia… - Journal of Enzyme …, 2023 - Taylor & Francis
The colchicine binding site of tubulin is a promising target for discovering novel antitumour
agents. Previously, we identified 2-aryl-4-amide-quinoline derivatives displayed moderate …

[HTML][HTML] Organotin benzohydroxamate derivatives (OTBH) target colchicine-binding site exerting potent antitumor activity both in vitro and vivo revealed by quantitative …

J Song, S Liu, Y Ren, X Zhang, B Zhao, X Wang… - European Journal of …, 2023 - Elsevier
The activity of four typical organotin benzohydroxamate compounds (OTBH) with the
different electronegativity of fluorine and chlorine atoms was assessed both in vitro and in …

It's ok to be outnumbered–sub-stoichiometric modulation of homomeric protein complexes

YN Dimitrova, JA Gutierrez, K Huard - RSC Medicinal Chemistry, 2023 - pubs.rsc.org
An arsenal of molecular tools with increasingly diversified mechanisms of action is being
developed by the scientific community to enable biological interrogation and pharmaceutical …

Structural basis of microtubule depolymerization by the kinesin-like activity of HIV-1 Rev

E Eren, NR Watts, D Randazzo, I Palmer, DL Sackett… - Structure, 2023 - cell.com
HIV-1 Rev is an essential regulatory protein that transports unspliced and partially spliced
viral mRNAs from the nucleus to the cytoplasm for the expression of viral structural proteins …