Progress of tubulin polymerization activity detection methods

T Zhu, SH Wang, D Li, SY Wang, X Liu, J Song… - Bioorganic & Medicinal …, 2021 - Elsevier
Tubulin, an important target in tumor therapy, is one of the hotspots in the field of
antineoplastic drugs in recent years, and it is of great significance to design and screen new …

Blocking blood flow to solid tumors by destabilizing tubulin: an approach to targeting tumor growth

MJ Pérez-Pérez, EM Priego, O Bueno… - Journal of medicinal …, 2016 - ACS Publications
The unique characteristics of the tumor vasculature offer the possibility to selectively target
tumor growth and vascularization using tubulin-destabilizing agents. Evidence accumulated …

Design, synthesis, and evaluation of in vitro and in vivo anticancer activity of 4-substituted coumarins: a novel class of potent tubulin polymerization inhibitors

D Cao, Y Liu, W Yan, C Wang, P Bai… - Journal of medicinal …, 2016 - ACS Publications
In this paper, a series of novel 4-substituted coumarin derivatives were synthesized. Among
these compounds 34, 39, 40, 43, 62, 65, and 67 exhibited significant antiproliferative activity …

Design, synthesis, and antitumor efficacy of substituted 2-amino [1, 2, 4] triazolopyrimidines and related heterocycles as dual inhibitors for microtubule polymerization …

L Chen, Y Hu, Z Lu, Z Lin, L Li, JQ Wu… - Journal of Medicinal …, 2023 - ACS Publications
Preclinical and clinical studies have demonstrated the synergistic effect of microtubule-
targeting agents in combination with Janus kinase 2 (JAK2) inhibitors, prompting the …

Design, synthesis, biological assessment, and in-silico studies of 1, 2, 4-triazolo [1, 5-a] pyrimidine derivatives as tubulin polymerization inhibitors

HS Mohamed, NH Amin, MT El-Saadi… - Bioorganic …, 2022 - Elsevier
Abstract A series of 1, 2, 4-triazolo [1, 5-a] pyrimidine derivatives have been designed and
synthesized as combretastatin CA-4 analogs. They were screened for anticancer and tubulin …

Advances in antitumor research of CA-4 analogs carrying quinoline scaffold

C Wang, J Chang, S Yang, L Shi, Y Zhang… - Frontiers in …, 2022 - frontiersin.org
Combretastatin A-4 (CA-4) is a potent inhibitor of tubulin polymerization and a colchicine
binding site inhibitor (CBSI). The structure-activity relationship study of CA-4 showed that the …

Imidazo [4, 5-b] pyridine derived tubulin polymerization inhibitors: Design, synthesis, biological activity in vitro and computational analysis

I Boček, L Hok, L Persoons, D Daelemans… - Bioorganic …, 2022 - Elsevier
Abstract Imidazo [4, 5-b] pyridine derived acrylonitriles were synthesized and explored for
their in vitro antiproliferative effect on a diverse human cancer cell line panel. Three …

Reversible binding of the anticancer drug KXO1 (tirbanibulin) to the colchicine-binding site of β-tubulin explains KXO1's low clinical toxicity

L Niu, J Yang, W Yan, Y Yu, Y Zheng, H Ye… - Journal of Biological …, 2019 - ASBMB
KXO1 (tirbanibulin or KX2–391) is as a non-ATP-competitive inhibitor of SRC proto-
oncogene nonreceptor tyrosine kinase (SRC) and is being clinically investigated for the …

N-substituted benzimidazole acrylonitriles as in vitro tubulin polymerization inhibitors: Synthesis, biological activity and computational analysis

N Perin, L Hok, A Beč, L Persoons, E Vanstreels… - European journal of …, 2021 - Elsevier
We present the design, synthesis and biological activity of novel N-substituted
benzimidazole based acrylonitriles as potential tubulin polymerization inhibitors. Their …

Design, synthesis and biological evaluation of indole-based [1, 2, 4] triazolo [4, 3-a] pyridine derivatives as novel microtubule polymerization inhibitors

CJ Wu, JQ Wu, Y Hu, S Pu, Y Lin, Z Zeng, J Hu… - European Journal of …, 2021 - Elsevier
A series of indole-based [1, 2, 4] triazolo [4, 3-a] pyridine derivatives was designed and
synthesized as novel microtubulin polymerization inhibitors by using a conformational …