Drug intelligence / Profile preview

Compound 4h

Development stage
Preclinical
Modality
Small Molecules
Administration
Intragastric
01

Overview

Compound 4h is a non-specific research designation for small molecule drug candidates identified in various medicinal chemistry studies. In the context of oncology research, it refers to at least two distinct chemical entities described in the literature. One version is an N-arylidene hydrazinyl Schiff base derivative containing a trimethoxyphenyl (TMP) ring, which functions as a tubulin polymerization inhibitor. This compound has demonstrated potent cytotoxic activity against the MDA-MB-231 breast cancer cell line by disrupting the dynamic equilibrium of alpha and beta-tubulin, leading to cell cycle arrest and apoptosis. A second version is a 1,3,4-thiadiazole derivative bearing a pyridine moiety, which has shown significant in vitro activity against human colon carcinoma (HCT-116) and hepatocellular carcinoma (HepG-2) cell lines. Molecular docking studies suggest this version acts as an inhibitor of the Epidermal Growth Factor Receptor (EGFR) tyrosine kinase. Both compounds are currently in the early stages of preclinical investigation and are used as lead candidates for further development.

02

Targets

TUBA (Tubulin alpha/beta dimer)EGFR (Epidermal growth factor receptor)

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