ArticleACS medicinal chemistry letters2015
Structural Optimization of Indole Derivatives Acting at Colchicine Binding Site as Potential Anticancer Agents.
Article in ACS medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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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.
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Who cites it
25 citing papers in PubMed.
- A Phase Ib/II Study of Sabizabulin, a Novel Oral Cytoskeleton Disruptor, in Men with Metastatic Castration-resistant Prostate Cancer with Progression on an Androgen Receptor-targeting Agent.Clinical cancer research : an official journal of the American Association for Cancer Research · 2022Trial
- SCHEMBL4796824: a multifaceted antitumor agent targeting microtubule dynamics, DNA damage, and Wnt/β-catenin signaling in ovarian cancer cells.Journal of ovarian research · 2026Article
- Design and synthesis of novel 4-aryl-2-benzoyl-imidazoles as colchicine binding site inhibitors.European journal of medicinal chemistry · 2025Article
- 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
- Fused Imidazopyrazine-Based Tubulin Polymerization Inhibitors Inhibit Neuroblastoma Cell Function.ACS medicinal chemistry letters · 2023Article
- A Facile Synthesis and Molecular Characterization of Certain New Anti-Proliferative Indole-Based Chemical Entities.International journal of molecular sciences · 2023Article
- 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
- Molecular interactions at the colchicine binding site in tubulin: An X-ray crystallography perspective.Drug discovery today · 2022Review
- Discovery of Novel DiarylamideMolecules (Basel, Switzerland) · 2021Article
- Nanoformulation design and therapeutic potential of a novel tubulin inhibitor in pancreatic cancer.Journal of controlled release : official journal of the Controlled Release Society · 2021Article
- Colchicine-Binding Site Inhibitors from Chemistry to Clinic: A Review.Pharmaceuticals (Basel, Switzerland) · 2020Review
- Article
- A new,Chemical science · 2019Article
- Nanoparticulate delivery of potent microtubule inhibitor for metastatic melanoma treatment.Journal of controlled release : official journal of the Controlled Release Society · 2019Article
- Polymeric Micellar Delivery of Novel Microtubule Destabilizer and Hedgehog Signaling Inhibitor for Treating Chemoresistant Prostate Cancer.The Journal of pharmacology and experimental therapeutics · 2019Article
- Colchicine Binding Site Agent DJ95 Overcomes Drug Resistance and Exhibits Antitumor Efficacy.Molecular pharmacology · 2019Article
- Current advances of tubulin inhibitors as dual acting small molecules for cancer therapy.Medicinal research reviews · 2019Review
- Design, synthesis and biological evaluation of selective survivin inhibitors.Journal of biomedical research · 2019Article
- Structural Modification of the 3,4,5-Trimethoxyphenyl Moiety in the Tubulin Inhibitor VERU-111 Leads to Improved Antiproliferative Activities.Journal of medicinal chemistry · 2018Article
Corrections and comments
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Authors and funding
4 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A new series of indole analogues based on our earlier lead compound, 2-(1H-indol-5-yl)-4-(3,4,5-trimethoxyphenyl)-1H-imidazo[4,5-c]pyridine (42), was prepared as tubulin inhibitors in an effort to find a molecule with improved cytotoxic potency and metabolic stability. A series of indolyl-imidazopyridines (IIP) were synthesized and exhibited potent tubulin polymerization inhibitory activity with potent IC50 values ranging from 3 to 175 nM against a panel of human melanoma and prostate cancer cell lines. Among these compounds, the 6-indolyl compound 43 showed improved cytotoxic potency (average IC50 of 9.75 nM vs 55.75 nM) and metabolic stability in human liver microsomes (half-life time was 56.3 min vs. 45.4 min) as compared to previously reported 42. It was also shown to be effective against P-glycoprotein (P-gp) mediated multiple drug resistance (MDR) and taxol resistance.
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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.