An overview of tubulin inhibitors that interact with the colchicine binding site

Y Lu, J Chen, M Xiao, W Li, DD Miller - Pharmaceutical research, 2012 - Springer
Tubulin dynamics is a promising target for new chemotherapeutic agents. The colchicine
binding site is one of the most important pockets for potential tubulin polymerization …

The chemistry of heterocycles in the 21st century

VN Charushin, EV Verbitskiy, ON Chupakhin… - Uspekhi Khimii, 2024 - mathnet.ru
The chemistry of heterocyclic compounds has traditionally been and remains a bright area of
chemical science in Russia. This is due to the fact that many heterocycles find the widest …

Recent advances in trimethoxyphenyl (TMP) based tubulin inhibitors targeting the colchicine binding site

L Li, S Jiang, X Li, Y Liu, J Su, J Chen - European journal of medicinal …, 2018 - Elsevier
Microtubules (composed of α-and β-tubulin heterodimers) play a pivotal role in mitosis and
cell division, and are regarded as an excellent target for chemotherapeutic agents to treat …

Structures of a diverse set of colchicine binding site inhibitors in complex with tubulin provide a rationale for drug discovery

Y Wang, H Zhang, B Gigant, Y Yu, Y Wu… - The FEBS …, 2016 - Wiley Online Library
Microtubules are dynamic assemblies of αβ‐tubulin heterodimers and have been
recognized as highly attractive targets for cancer chemotherapy. A broad range of agents …

Anti‐mitotic activity of colchicine and the structural basis for its interaction with tubulin

B Bhattacharyya, D Panda, S Gupta… - Medicinal research …, 2008 - Wiley Online Library
In this review, an attempt has been made to throw light on the mechanism of action of
colchicine and its different analogs as anti‐cancer agents. Colchicine interacts with tubulin …

Destruction of tumor vasculature by vascular disrupting agents in overcoming the limitation of EPR effect

Z Liu, Y Zhang, N Shen, J Sun, Z Tang… - Advanced Drug Delivery …, 2022 - Elsevier
Nanomedicine greatly improves the efficiency in the delivery of antitumor drugs into the
tumor, but insufficient tumoral penetration impairs the therapeutic efficacy of most …

Recent developments in tubulin polymerization inhibitors: an overview

R Kaur, G Kaur, RK Gill, R Soni, J Bariwal - European journal of medicinal …, 2014 - Elsevier
Microtubules are protein biopolymers formed through polymerization of heterodimers of α-
and β-tubulins. Disruption of microtubules can induce cell cycle arrest in G 2-M phase and …

Discovery of new quinolines as potent colchicine binding site inhibitors: Design, synthesis, docking studies, and anti-proliferative evaluation

M Hagras, MA El Deeb, HSA Elzahabi… - Journal of Enzyme …, 2021 - Taylor & Francis
Discovering of new anticancer agents with potential activity against tubulin polymerisation is
still a promising approach. Colchicine binding site inhibitors are the most relevant anti …

Colchicine alkaloids and synthetic analogues: current progress and perspectives

IA Gracheva, ES Shchegravina… - Journal of medicinal …, 2020 - ACS Publications
Colchicine, the main alkaloid of Colchicum autumnale, is one of the most famous natural
molecules. Although colchicine belongs to the oldest drugs (in use since 1500 BC), its …

Design and synthesis of novel benzoazoninone derivatives as potential CBSIs and apoptotic inducers: in vitro, in vivo, molecular docking, molecular dynamics, and …

MM Hammouda, AA Elmaaty, MS Nafie… - Bioorganic …, 2022 - Elsevier
Apparently, tubulin inhibitors binding to the colchicine-binding site (CBS) currently have
outstanding attention for cancer treatment. So, a series of benzo [b] azonin-2-one derivatives …