ArticleJournal of medicinal chemistry2021
X-ray Crystallography-Guided Design, Antitumor Efficacy, and QSAR Analysis of Metabolically Stable Cyclopenta-Pyrimidinyl Dihydroquinoxalinone as a Potent Tubulin Polymerization Inhibitor.
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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 18 papers.
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Who cites it
18 citing papers in PubMed.
- Therapeutic potential of colchicine-binding site inhibitors in breast cancer brain metastasis.Cancer letters · 2026Review
- Structural and biochemical insights into the antibiofilm activity of cationic lipoamino acid ester against methicillin-resistantRSC advances · 2026Article
- Discovery of Potent and Brain-Penetrable Tubulin Inhibitors that Effectively Suppress Breast Cancer Brain Metastasis.Molecular cancer therapeutics · 2026Article
- Novel Triazoloquinoxaline-Based Tubulin Polymerization Inhibitor Induces Necroptosis and Significantly Inhibits Metastatic Melanoma Tumor Growth.Journal of medicinal chemistry · 2026Article
- Dual targeting of oncogenic microtubules and mitochondria in PDAC.Oncoscience · 2026Article
- A Pyrimidine-Based Tubulin Inhibitor Shows Potent Anti-Glioblastoma Activity In Vitro and In Vivo.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Pyrimidine hybrids withFuture medicinal chemistry · 2025Review
- Colchicine Binding Site Tubulin Inhibitors Impair Vincristine-Resistant Neuroblastoma Cell Function.Molecules (Basel, Switzerland) · 2025Article
- Biological activity of a stable 6-aryl-2-benzoyl-pyridine colchicine-binding site inhibitor, 60c, in metastatic, triple-negative breast cancer.Cancer letters · 2024Article
- Selective isoxazolopyrimidine PAT1 (SLC26A6) inhibitors for therapy of intestinal disorders.RSC medicinal chemistry · 2023Article
- Verubulin (Azixa) Analogues with Increased Saturation: Synthesis, SAR and Encapsulation in Biocompatible Nanocontainers Based on CaPharmaceuticals (Basel, Switzerland) · 2023Article
- Fused Imidazopyrazine-Based Tubulin Polymerization Inhibitors Inhibit Neuroblastoma Cell Function.ACS medicinal chemistry letters · 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
- Consensus Virtual Screening Protocol Towards the Identification of Small Molecules Interacting with the Colchicine Binding Site of the Tubulin-microtubule System.Molecular informatics · 2023Article
- Synthesis, Characterisation and Mechanism of Action of Anticancer 3-Fluoroazetidin-2-ones.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
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Authors and funding
17 authors.
Souvik BanerjeeDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.ORCID 0000-0002-7811-2577
Foyez MahmudDepartment 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.
Lingling MaDepartment of Respiratory and Critical Care Medicine, Targeted Tracer Research and Development Laboratory, West China Hospital, Sichuan University, Chengdu 610041, China.
Mi-Kyung YunDepartment of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
Sayo O FakayodeDepartment of Physical Sciences, College of STEM, University of Arkansas Fort Smith, Fort Smith, Arkansas 72913, United States.
Kinsie E ArnstDepartment of Pharmaceutical Sciences, College of Pharmacy, 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.
Hao ChenDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.
Zhongzhi WuDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.
Pradeep B LukkaDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.ORCID 0000-0001-8034-7810
Keyur ParmarDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.
Bernd MeibohmDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.ORCID 0000-0003-3923-3648
Stephen W WhiteDepartment of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
Yuxi WangDepartment of Respiratory and Critical Care Medicine, Targeted Tracer Research and Development Laboratory, West China Hospital, Sichuan University, Chengdu 610041, China.ORCID 0000-0002-4056-5829
Wei LiDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.ORCID 0000-0002-9522-4474
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
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
$325kMass Spectrometer for Small Molecule Drug DevelopmentS10OD016226 · OD · UNIVERSITY OF TENNESSEE HEALTH SCI CTR · PI MEIBOHM, BERND · 2014 to 2014
$316kAcquisition 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 OD010678NIH HHS S10 OD016226
Abstract
Small molecules that interact with the colchicine binding site in tubulin have demonstrated therapeutic efficacy in treating cancers. We report the design, syntheses, and antitumor efficacies of new analogues of pyridopyrimidine and hydroquinoxalinone compounds with improved drug-like characteristics. Eight analogues,
Indexed as
AnimalsAntineoplastic AgentsApoptosisCell CycleCell Line, TumorCell SurvivalCrystallography, X-RayDrug DesignDrug Resistance, NeoplasmFemaleHumansMaleMiceQuantitative Structure-Activity RelationshipQuinoxalinesTubulin ModulatorsAntineoplastic AgentsQuinoxalinesTubulin Modulators
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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.