ArticleCancer letters2023
SB226, an inhibitor of tubulin polymerization, inhibits paclitaxel-resistant melanoma growth and spontaneous metastasis.
Article in Cancer letters, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed.
- Conformationally constrained 6‑aryl‑1‑(3,4,5‑trimethoxyphenyl)-1Journal of enzyme inhibition and medicinal chemistry · 2026Article
- QW-5-70 targets the colchicine site and demonstrates antitumor activity in P-gp-overexpressing cancer models.Molecular cancer therapeutics · 2026Article
- Novel Triazoloquinoxaline-Based Tubulin Polymerization Inhibitor Induces Necroptosis and Significantly Inhibits Metastatic Melanoma Tumor Growth.Journal of medicinal chemistry · 2026Article
- A Pyrimidine-Based Tubulin Inhibitor Shows Potent Anti-Glioblastoma Activity In Vitro and In Vivo.Pharmaceuticals (Basel, Switzerland) · 2025Article
- lncRNA RP11-199F11.2 promotes high-grade serous ovarian cancer cell proliferation by regulating cuproptosis through FDX1.Scientific reports · 2025Article
- Colchicine-BODIPY Probes: Evidence for the Involvement of Intracellular Membranes in the Targeting of Colchicine to Tubulin.ACS pharmacology & translational science · 2025Article
- Pyrimidine hybrids withFuture medicinal chemistry · 2025Review
- Paclitaxel in colon cancer management: from conventional chemotherapy to advanced nanocarrier delivery systems.Naunyn-Schmiedeberg's archives of pharmacology · 2024Review
- Biological activity of a stable 6-aryl-2-benzoyl-pyridine colchicine-binding site inhibitor, 60c, in metastatic, triple-negative breast cancer.Cancer letters · 2024Article
- The Circular RNA circFOXK2 Enhances the Tumorigenesis of Non-Small Cell Lung Cancer Through the miR-149-3p/IL-6 Axis.Biochemical genetics · 2024Article
- Fused Imidazopyrazine-Based Tubulin Polymerization Inhibitors Inhibit Neuroblastoma Cell Function.ACS medicinal chemistry letters · 2023Article
- Antiproliferative and Tubulin-Destabilising Effects of 3-(Prop-1-en-2-yl)azetidin-2-Ones and Related Compounds in MCF-7 and MDA-MB-231 Breast Cancer Cells.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Targeting CD73 increases therapeutic response to immunogenic chemotherapy by promoting dendritic cell maturation.Cancer immunology, immunotherapy : CII · 2023Article
- S-72, a Novel Orally Available Tubulin Inhibitor, Overcomes Paclitaxel Resistance via Inactivation of the STING Pathway in Breast Cancer.Pharmaceuticals (Basel, Switzerland) · 2023Article
Corrections and comments
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Authors and funding
13 authors.
Funding
Abstract
Extensive preclinical studies have shown that colchicine-binding site inhibitors (CBSIs) are promising drug candidates for cancer therapy. Although numerous CBSIs were generated and evaluated, but so far the FDA has not approved any of them due to undesired adverse events or insufficient efficacies. We previously reported two very potent CBSIs, the dihydroquinoxalinone compounds 5 m and 5t. In this study, we further optimized the structures of compounds 5 m and 5t and integrated them to generate a new analog, SB226. X-ray crystal structure studies and a tubulin polymerization assay confirmed that SB226 is a CBSI that could disrupt the microtubule dynamics and interfere with microtubule assembly. Biophysical measurements using surface plasmon resonance (SPR) spectroscopy verified the high binding affinity of SB226 to tubulin dimers. The in vitro studies showed that SB226 possessed sub-nanomolar anti-proliferative activities with an average IC
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