Viswanathan, Anisha published the artcile2-(2-(2,4-Dioxopentan-3-ylidene)hydrazinyl)benzonitrile as novel inhibitor of receptor tyrosine kinase and PI3K/AKT/mTOR signaling pathway in glioblastoma, Related Products of nitriles-buliding-blocks, the main research area is arylhydrazone preparation anticancer activity tyrosine kinase mol docking.
The authors report the synthesis of 23 arylhydrazones of active methylene compounds (AHAMCs) compounds, e.g., I, and their anti-proliferative activity against GBM cell lines LN229 and U87. 2-[2-(2,4-Dioxopentan-3-ylidene)hydrazinyl]benzonitrile (II) was identified as the most active anti-neoplastic compound with the IC50 value ranging of 87 μM – 107 μM. Mol. docking simulations of the synthesized compounds into the active site of tyrosine receptor kinase A (TrkA) demonstrated a strong binding affinity with II and concurs well with the obtained biol. results. II was found to be a neg. regulator of PI3K/Akt/mTOR pathway and an enhancer of p53 expression. In addition, GBM cells treated with II exhibited the down-regulation of cyclins, cyclin-dependent kinases and other key mols. involved in cell cycle such as CCNE, E2F, CCND, CDK6, indicating that II induces cell cycle arrest at G1/S. II also exerted its apoptotic effects independent of caspase 3/7 activity in both cell lines. In U87 cells, II induced oxidative effects, whereas LN229 cells annulled oxidative stress. The study thus concludes that II, being a neg. modulator of RTKs and cell cycle inhibitor, may represent a novel class of anti-GBM drugs.
European Journal of Medicinal Chemistry published new progress about Active methylene compounds Role: RCT (Reactant), RACT (Reactant or Reagent). 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Related Products of nitriles-buliding-blocks.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts