Publications by authors named "Iin Narwanti"

Cell division cycle 25 (CDC25) phosphatase is a key cell cycle regulator whose overexpression is linked to tumor malignancy and poor prognosis. Its inhibition suppresses cancer cell growth and induces cell death, making it a promising therapeutic target. In this study, we aimed to develop novel CDC25 inhibitors with therapeutic potential.

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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.
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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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Article Synopsis
  • 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.
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