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 …

Disrupting tumour blood vessels

GM Tozer, C Kanthou, BC Baguley - Nature Reviews Cancer, 2005 - nature.com
Low-molecular-weight vascular-disrupting agents (VDAs) cause a pronounced shutdown in
blood flow to solid tumours, resulting in extensive tumour-cell necrosis, while they leave the …

Discovery of DRP-104, a tumor-targeted metabolic inhibitor prodrug

R Rais, KM Lemberg, L Tenora, ML Arwood, A Pal… - Science …, 2022 - science.org
6-Diazo-5-oxo-l-norleucine (DON) is a glutamine antagonist that suppresses cancer cell
metabolism but concurrently enhances the metabolic fitness of tumor CD8+ T cells. DON …

Medicinal chemistry of combretastatin A4: present and future directions

GC Tron, T Pirali, G Sorba, F Pagliai… - Journal of medicinal …, 2006 - ACS Publications
A growing solid tumor relies on a developing vasculature to meet its needs in terms of
oxygen, nutrients, depuration, etc. This implies that if the vascular bed that has developed …

[图书][B] Anticancer agents from natural products

GM Cragg, DGI Kingston, DJ Newman - 2005 - taylorfrancis.com
Plants, marine organisms, and microorganisms have evolved complex chemical defense
and signaling systems that are designed to protect them from predators and provide other …

Colchicine-binding site inhibitors from chemistry to clinic: a review

EC McLoughlin, NM O'Boyle - Pharmaceuticals, 2020 - mdpi.com
It is over 50 years since the discovery of microtubules, and they have become one of the
most important drug targets for anti-cancer therapies. Microtubules are predominantly …

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 …

Design and discovery of new antiproliferative 1, 2, 4-triazin-3 (2H)-ones as tubulin polymerization inhibitors targeting colchicine binding site

IH Eissa, MA Dahab, MK Ibrahim, NA Alsaif… - Bioorganic …, 2021 - Elsevier
Thirty-five new colchicine binding site inhibitors have been designed and synthesized based
on the 1, 2, 4-triazin-3 (2 H)-one nucleus. Such molecules were synthesized through a …

Vascular disrupting agents

JW Lippert III - Bioorganic & medicinal chemistry, 2007 - Elsevier
A clear definition for vascular targeting agents (VTAs) and vascular disrupting agents (VDAs)
has separated the two as distinct methods of cancer treatment. VDAs differ from VTAs …

Vascular disrupting agents in cancer therapy

R Smolarczyk, J Czapla, M Jarosz-Biej… - European Journal of …, 2021 - Elsevier
Tumor blood vessel formation is a key process for tumor expansion. Tumor vessels are
abnormal and differ from normal vessels in architecture and components. Besides oxygen …