Publications by authors named "Bidyadhar Sethy"
Article Synopsis
- Triple-negative breast cancer (TNBC) is difficult to treat due to its aggressive nature and limited effective therapies, prompting the need for new treatments.
- The study developed dual inhibitors targeting CDC25 and HDACs by combining specific molecular structures, showing that one compound, 18A, was particularly effective against TNBC cells while sparing non-cancerous cells.
- 18A demonstrated strong cytotoxic effects, inhibited key cell cycle proteins, triggered DNA damage, and induced cell death, highlighting its potential as a promising targeted therapy for TNBC that requires further research.
Disruptor of telomeric silencing 1-like (DOT1L) is a key hub in histone lysine methyltransferase and an attractive therapeutic target for treating hematological malignancies including acute myeloid leukemia (AML). In this study, we report the design and synthesis of a new series of adenosine derivatives as DOT1L inhibitors by accommodating a basic linker piperidine-4-ylmethyl motif to respective aryl-urea/benzimidazole scaffolds. The anti-DOT1L enzyme activity analysis demonstrated that compounds 8, 12, and 13 strongly suppressed DOT1L activity with IC values ranging from 0.
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- Precise control of the cell cycle is crucial for maintaining cell identity and preventing issues like tumor formation, with CDC25 phosphatases playing a key role in regulating cyclin-dependent kinases (CDKs).
- A series of derivatives of the CDC25 inhibitor, NSC663284, showed enhanced potency against colorectal cancer cells, particularly the 6-isomer of 5,8-quinolinedione (compound 6b), which exhibited strong antiproliferative activity.
- Compound 6b not only blocked cell cycle progression and induced DNA damage but also triggered apoptosis in cancer cells, highlighting its potential as a candidate for further development as an anti-colorectal cancer agent.
The Michael addition reaction is a spontaneous and quick chemical reaction that is widely applied in various fields. This reaction is performed by conjugating an addition of nucleophiles with α, β-unsaturated carbonyl compounds, resulting in the bond formation of C-N, C-S, C-O, and so on. In the development of molecular materials, the Michael addition is not only used to synthesize chemical compounds but is also involved in the mechanism of drug action.
View Article and Find Full Text PDFModulating epigenetic modification has been recognized for over a decade as an effective therapeutic approach to cancer and many studies of histone deacetylase (HDAC), one of the best known epigenetic modulators, have been published. HDAC modulates cell proliferation and angiogenesis and plays an essential role in cell growth. Research shows that up-regulated HDACs are present in many cancer types and synthetic or natural HDAC inhibitors have been used to silence overregulated HDACs.
View Article and Find Full Text PDFInfluenza A viruses (IAVs) have caused worldwide epidemics and pandemics by reassortment and generation of drug-resistant mutants, which render antivirals and current vaccinations no longer usable. In this study, an itaconic acid derivative 1 was identified from a chemical library of 20 000 compounds, by performing a cell-based screening assay, as a lead agent exhibiting anti-influenza A activity. Accordingly, a series of itaconic acid derivatives were designed and synthesized by adopting a rational design strategy to obtain more potent anti-influenza agents.
View Article and Find Full Text PDFAim: No antiviral medications are currently approved to treat enterovirus (EV)-associated disease or prevent EV infection.
Methods: In this study, a series of probenecid derivatives were designed via a rational strategy and synthesized to obtain more potent anti-EV agents.
Results: Compounds 8 and 24 exhibited the most potent activity against EV D68 and A71, with half maximal effective concentration (EC) values of 2.