Drug intelligence / Profile preview

S009-131

Development stage
Preclinical
Lead developer
CSIR-Central Drug Research Institute
Modality
Small Molecules
Administration
Oral
01

Overview

S009-131 is a synthetic coumarin-chalcone hybrid molecule investigated for its anti-tumor and anti-proliferative properties, particularly in cervical carcinoma. It functions by inducing apoptosis through the intrinsic mitochondrial pathway and arresting the cell cycle at the G2/M phase. Mechanistically, it increases the Bax/Bcl-2 ratio, generates intracellular reactive oxygen species (ROS), and depletes mitochondrial transmembrane potential, leading to the release of cytochrome c and activation of caspases 9, 3, and 7. Additionally, it upregulates tumor suppressor protein p53 and its transcriptional target PUMA. In vivo studies have demonstrated its efficacy in regressing HeLa cell xenograft tumors when administered orally.

Other names
coumarin-chalcone hybrid S009-131
02

Targets

MDM2 (Mouse double minute 2 homolog)DNA

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