ArticleJournal of medicinal chemistry2014
Design, synthesis, and biological evaluation of novel pyridine-bridged analogues of combretastatin-A4 as anticancer agents.
Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
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Who cites it
32 citing papers in PubMed.
- Nicotinonitrile based dual inhibitors of tubulin and topoisomerase II exhibit potent anticancer activity.Scientific reports · 2026Article
- Synthesis and Antiproliferative Activity against Melanoma Cells of New Heterocyclic Hybrids Based on Pyridine and Pyrimidine Scaffolds.Current medicinal chemistry · 2026Article
- Recent Advancements in the Development of HDAC/Tubulin Dual-Targeting Inhibitors.Pharmaceuticals (Basel, Switzerland) · 2025Review
- The Structure-Antiproliferative Activity Relationship of Pyridine Derivatives.International journal of molecular sciences · 2024Review
- PM534, an Optimized Target-Protein Interaction Strategy through the Colchicine Site of Tubulin.Journal of medicinal chemistry · 2024Article
- Clickable bisreactive small gold nanoclusters for preparing multifunctionalized nanomaterials: application to photouncaging of an anticancer molecule.Chemical science · 2024Article
- Synthesis and Selective Anticancer Activity Evaluation of 2-phenylacrylonitrile Derivatives as Tubulin Inhibitors.Current medicinal chemistry · 2024Article
- Lignin-Based Catalysts for C-C Bond-Forming Reactions.Molecules (Basel, Switzerland) · 2023Review
- Nitrogen Containing Heterocycles as Anticancer Agents: A Medicinal Chemistry Perspective.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Synthesis and bioactive evaluation ofRSC medicinal chemistry · 2023Article
- Design, synthesis and biological evaluation of novel diarylpyridine derivatives as tubulin polymerisation inhibitors.Journal of enzyme inhibition and medicinal chemistry · 2022Article
- Design and synthesis of new trimethoxylphenyl-linked combretastatin analogues loaded on diamond nanoparticles as a panel for ameliorated solubility and antiproliferative activity.Journal of enzyme inhibition and medicinal chemistry · 2022Article
- Article
- Synthesis and characterization of novel combretastatin analogues of 1,1-diaryl vinyl sulfones, with antiproliferative potential via in-silico and in-vitro studies.Scientific reports · 2022Article
- Design, synthesis, docking study and anticancer evaluation of new trimethoxyphenyl pyridine derivatives as tubulin inhibitors and apoptosis inducers.RSC advances · 2021Article
- β-Carboline-based molecular hybrids as anticancer agents: a brief sketch.RSC medicinal chemistry · 2021Review
- Synthesis, Biological Evaluation, and Molecular Docking of Arylpyridines as Antiproliferative Agent Targeting Tubulin.ACS medicinal chemistry letters · 2020Article
- Colchicine-Binding Site Inhibitors from Chemistry to Clinic: A Review.Pharmaceuticals (Basel, Switzerland) · 2020Review
- A novel and robust heterogeneous Cu catalyst using modified lignosulfonate as support for the synthesis of nitrogen-containing heterocycles.Beilstein journal of organic chemistry · 2020Article
- Current advances of tubulin inhibitors as dual acting small molecules for cancer therapy.Medicinal research reviews · 2019Review
Corrections and comments
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Authors and funding
8 authors.
Funding
Abstract
A series of novel pyridine-bridged analogues of combretastatin-A4 (CA-4) were designed and synthesized. As expected, the 4-atom linker configuration retained little cytotoxicities in the compounds 2e, 3e, 3g, and 4i. Activities of the analogues with 3-atom linker varied widely depending on the phenyl ring substitutions, and the 3-atom linker containing nitrogen represents the more favorable linker structure. Among them, three analogues (4h, 4s, and 4t) potently inhibited cell survival and growth, arrested cell cycle, and blocked angiogenesis and vasculature formation in vivo in ways comparable to CA-4. The superposition of 4h and 4s in the colchicine-binding pocket of tubulin shows the binding posture of CA-4, 4h, and 4s are similar, as confirmed by the competitive binding assay where the ability of the ligands to replace tubulin-bound colchicine was measured. The binding data are consistent with the observed biological activities in antiproliferation and suppression of angiogenesis but are not predictive of their antitubulin polymerization activities.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.