ArticleEuropean journal of medicinal chemistry2014
Discovery of potent anticancer agent HJC0416, an orally bioavailable small molecule inhibitor of signal transducer and activator of transcription 3 (STAT3).
Article in European 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 21 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
21 citing papers in PubMed.
- Room-Temperature Helix-to-Disc Conversion of Thia[6]helicene S,S-Dioxides to Coronene via In Situ Phenoxide Anion Generation.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Article
- A Novel Ageladine A Derivative Acts as a STAT3 Inhibitor and Exhibits Potential Antitumor Effects.International journal of molecular sciences · 2023Article
- STAT family of transcription factors in breast cancer: Pathogenesis and therapeutic opportunities and challenges.Seminars in cancer biology · 2022Review
- Induction of Genes Implicated in Stress Response and Autophagy by a Novel Quinolin-8-yl-nicotinamide QN523 in Pancreatic Cancer.Journal of medicinal chemistry · 2022Article
- Structure-activity relationship studies on O-alkylamino-tethered salicylamide derivatives with various amino acid linkers as potent anticancer agents.European journal of medicinal chemistry · 2022Article
- HJC0416 Attenuates Fibrogenesis in Activated Hepatic Stellate Cells via STAT3 and NF-κB Pathways.The Journal of surgical research · 2021Article
- Hybrid Drugs-A Strategy for Overcoming Anticancer Drug Resistance?Molecules (Basel, Switzerland) · 2021Review
- JMX0207, a Niclosamide Derivative with Improved Pharmacokinetics, Suppresses Zika Virus Infection BothACS infectious diseases · 2020Article
- Discovery of New Apoptosis-Inducing Agents for Breast Cancer Based on Ethyl 2-Amino-4,5,6,7-Tetra Hydrobenzo[Molecules (Basel, Switzerland) · 2020Article
- Trioxolone Methyl, a Novel Cyano Enone-Bearing 18βH-Glycyrrhetinic Acid Derivative, Ameliorates Dextran Sulphate Sodium-Induced Colitis in Mice.Molecules (Basel, Switzerland) · 2020Article
- Small molecule inhibitors in pancreatic cancer.RSC medicinal chemistry · 2020Review
- Discovery of monocarbonyl curcumin-BTP hybrids as STAT3 inhibitors for drug-sensitive and drug-resistant breast cancer therapy.Scientific reports · 2017Article
- Discovery and development of natural product oridonin-inspired anticancer agents.European journal of medicinal chemistry · 2016Review
- BH4 domain of Bcl-2 as a novel target for cancer therapy.Drug discovery today · 2016Review
- STAT3 Inhibition Suppresses Hepatic Stellate Cell Fibrogenesis: HJC0123, a Potential Therapeutic Agent for Liver Fibrosis.RSC advances · 2016Article
- Novel 2-Carbonylbenzo[b]thiophene 1,1-Dioxide Derivatives as Potent Inhibitors of STAT3 Signaling Pathway.ACS medicinal chemistry letters · 2015Article
- The unusual suspects--innate lymphoid cells as novel therapeutic targets in IBD.Nature reviews. Gastroenterology & hepatology · 2015Review
- Evolution in medicinal chemistry of ursolic acid derivatives as anticancer agents.European journal of medicinal chemistry · 2015Review
- Evolutions in fragment-based drug design: the deconstruction-reconstruction approach.Drug discovery today · 2015Review
- Fas Signaling Promotes Gastric Cancer Metastasis through STAT3-Dependent Upregulation of Fascin.PloS one · 2015Article
Corrections and comments
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Authors and funding
12 authors.
Funding
Abstract
In a continuing effort to develop orally bioavailable small-molecule STAT3 inhibitors as potential therapeutic agents for human cancer, a series of novel diversified analogues based on our identified lead compound HJC0149 (1) (5-chloro-N-(1,1-dioxo-1H-1λ(6)-benzo[b]thiophen-6-yl)-2-hydroxybenzamide, Eur. J. Med. Chem. 2013, 62, 498-507) have been rationally designed, synthesized, and pharmacologically evaluated. Molecular docking studies and biological characterization supported our earlier findings that the O-alkylamino-tethered side chain on the hydroxyl group is an effective and essential structural determinant for improving biological activities and druglike properties of these molecules. Compounds with such modifications exhibited potent antiproliferative effects against breast and pancreatic cancer cell lines with IC50 values from low micromolar to nanomolar range. Among them, the newly discovered STAT3 inhibitor 12 (HJC0416) displayed an intriguing anticancer profile both in vitro and in vivo (i.p. & p.o.). More importantly, HJC0416 is an orally bioavailable anticancer agent as a promising candidate for further development.
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Registered trials
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