ArticleCell death & disease2014
SKLB-163, a new benzothiazole-2-thiol derivative, exhibits potent anticancer activity by affecting RhoGDI/JNK-1 signaling pathway.
Article in Cell death & disease, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 27 citations in OpenAlex.
- Synthetic strategies towards benzothiazole-based compounds of therapeutic potency: experimental, investigational and approved drugs.RSC advances · 2025Review
- Anticancer and Anti-Inflammatory Effects of Benzothiazole Derivatives Targeting NF-κB/COX-2/iNOS in a Hepatocellular Carcinoma Cell Line.Turkish journal of pharmaceutical sciences · 2025Article
- Underappreciated roles for Rho GDP dissociation inhibitors (RhoGDIs) in cell function: Lessons learned from the pancreatic islet β-cell.Biochemical pharmacology · 2022Review
- Betulinic acid induces apoptosis and suppresses metastasis in hepatocellular carcinoma cell lines in vitro and in vivo.Journal of cellular and molecular medicine · 2019Article
- Human Islet Response to Selected Type 1 Diabetes-Associated Bacteria: A Transcriptome-Based Study.Frontiers in immunology · 2019Article
- Antitumor and antimetastatic activities of a novel benzothiazole-2-thiol derivative in a murine model of breast cancer.Oncotarget · 2017Article
- Nifuroxazide exerts potent anti-tumor and anti-metastasis activity in melanoma.Scientific reports · 2016Article
- A novel inhibitor of Rho GDP-dissociation inhibitor α improves the therapeutic efficacy of paclitaxel in Lewis lung carcinoma.Biomedical reports · 2015Article
- Nifuroxazide induces apoptosis and impairs pulmonary metastasis in breast cancer model.Cell death & disease · 2015Article
- Caspase-9 mediates Puma activation in UCN-01-induced apoptosis.Cell death & disease · 2014Article
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Authors and funding
11 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Small-molecule inhibitors are an attractive therapeutic approach for most types of human cancers. SKLB-163, a novel benzothiazole-2-thiol derivative, was developed via computer-aided drug design and de novo synthesis. MTT assay showed it had potent anti-proliferative activity on various human cancer cells. Treatment of cancer cells with SKLB-163 induced obvious apoptosis and inhibited proliferation in vitro. SKLB-163 administered p.o. showed a marked antitumor activity in vivo. Proteomic techniques were employed to identify possible drug target proteins. The data showed molecular mechanism of action might be involved in downregulation of RhoGDI, which finally contributed to increased apoptosis and inhibited proliferation. These findings provided the potential value of SKLB-163 as a novel candidate antitumor drug.
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Registered trials
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