ArticleJournal of medicinal chemistry2021
Design, Synthesis, and Biological Evaluation of Stable Colchicine-Binding Site Tubulin Inhibitors 6-Aryl-2-benzoyl-pyridines as Potential Anticancer Agents.
Abstract read
In one paragraph
Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
0numbers the graph read from it
0cells of the map it votes in
21citing papers in PubMed
–field-weighted citation impact
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
21 citing papers in PubMed.
- Novel 6-aryl-1-(3,4,5-trimethoxyphenyl)-1Journal of enzyme inhibition and medicinal chemistry · 2026Article
- High-throughput ligand discovery in living cells using the cellular protein stability enhancement assay.Acta pharmaceutica Sinica. B · 2026Article
- QW-5-70 targets the colchicine site and demonstrates antitumor activity in P-gp-overexpressing cancer models.Molecular cancer therapeutics · 2026Article
- Design and synthesis of novel 4-aryl-2-benzoyl-imidazoles as colchicine binding site inhibitors.European journal of medicinal chemistry · 2025Article
- Recent Advances in Microtubule Targeting Agents for Cancer Therapy.Molecules (Basel, Switzerland) · 2025Review
- Synthesis and structure-activity relationship of boronic acid bioisosteres of combretastatin A-4 as anticancer agents.Bioorganic & medicinal chemistry · 2024Article
- Biological activity of a stable 6-aryl-2-benzoyl-pyridine colchicine-binding site inhibitor, 60c, in metastatic, triple-negative breast cancer.Cancer letters · 2024Article
- Synthesis and biological evaluation of structurally diverse 6-aryl-3-aroyl-indole analogues as inhibitors of tubulin polymerization.European journal of medicinal chemistry · 2024Article
- Discovery of potent tubulin inhibitors targeting the colchicine binding site via structure-based lead optimization and antitumor evaluation.Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Structural basis of microtubule depolymerization by the kinesin-like activity of HIV-1 Rev.Structure (London, England : 1993) · 2023Article
- Design, Synthesis, and Biological Evaluation of Pyrimidine Dihydroquinoxalinone Derivatives as Tubulin Colchicine Site-Binding Agents That Displayed Potent Anticancer Activity Both In Vitro and In Vivo.ACS pharmacology & translational science · 2023Article
- SB226, an inhibitor of tubulin polymerization, inhibits paclitaxel-resistant melanoma growth and spontaneous metastasis.Cancer letters · 2023Article
- It's ok to be outnumbered - sub-stoichiometric modulation of homomeric protein complexes.RSC medicinal chemistry · 2023Review
- Recent Advances of Tubulin Inhibitors Targeting the Colchicine Binding Site for Cancer Therapy.Biomolecules · 2022Review
- Design, Synthesis, Characterization, and Molluscicidal Activity Screening of New Nicotinonitrile Derivatives against Land Snails,Molecules (Basel, Switzerland) · 2022Article
- Sabizabulin, a Potent Orally Bioavailable Colchicine Binding Site Agent, Suppresses HER2+ Breast Cancer and Metastasis.Cancers · 2022Article
- Design, Synthesis and Biological Investigation of 2-Anilino Triazolopyrimidines as Tubulin Polymerization Inhibitors with Anticancer Activities.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Discovery of Putative Dual Inhibitor of Tubulin and EGFR by Phenotypic Approach on LASSBio-1586 Homologs.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Colchicine-Binding Site Agent CH-2-77 as a Potent Tubulin Inhibitor Suppressing Triple-Negative Breast Cancer.Molecular cancer therapeutics · 2022Article
- Design, Synthesis, and Biological Evaluation of Apcin-Based CDC20 Inhibitors.ACS medicinal chemistry letters · 2022Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
13 authors.
Hao ChenDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.
Shanshan DengDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.
Najah AlbadariDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.
Mi-Kyung YunDepartment of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
Sicheng ZhangDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.ORCID 0000-0003-3798-7550
Yong LiDepartment of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
Dejian MaDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.
Deanna N ParkeDepartment of Pathology, College of Medicine, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.
Lei YangDepartment of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
Tiffany N SeagrovesDepartment of Pathology, College of Medicine, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.
Stephen W WhiteDepartment of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
Duane D MillerDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.ORCID 0000-0002-6093-0985
Wei LiDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.ORCID 0000-0002-9522-4474
Funding
Targeting the colchicine site in tubulin for advanced melanomaR01CA148706 · NCI · UNIVERSITY OF TENNESSEE HEALTH SCI CTR · PI LI, WEI, MILLER, DUANE D · 2011 to 2025
$5.3MAcquisition of a Q-TOF Mass SpectrometerS10OD010678 · OD · UNIVERSITY OF TENNESSEE HEALTH SCI CTR · PI LI, WEI · 2012 to 2012
$325kAcquisition of a 400MHz Solution NMR System with an AutosamplerS10RR026377 · NCRR · UNIVERSITY OF TENNESSEE HEALTH SCI CTR · PI LI, WEI · 2010 to 2010
$253kNCI NIH HHS R01 CA148706NCRR NIH HHS S10 RR026377NIH HHS S10 OD010678
Abstract
We previously reported a potent tubulin inhibitor CH-2-77. In this study, we optimized the structure of CH-2-77 by blocking metabolically labile sites and synthesized a series of CH-2-77 analogues. Two compounds,
Indexed as
AnimalsAntineoplastic AgentsBinding SitesCell Line, TumorCell ProliferationDrug DesignDrug Screening Assays, AntitumorDrug StabilityFemaleG2 Phase Cell Cycle CheckpointsHumansMaleMiceMice, Inbred NODMice, SCIDMicrosomes, LiverAntineoplastic AgentsPyridinesTubulinTubulin Modulators
Identifiers
What OpenQuestion holds
Textmetadata
LicenceTDM
Read underepoch 390
Registered trials
None linked
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.