A series of new thiazole derivatives 3a–q were synthesized and tested against 60 cancer cell lines at the NCI, USA. Compound 3b showed the highest activity against PI3Kα with IC50 = 0.086 ± 0.005 μM and IC50 of 0.221 ± 0.014 μM against mTOR.
In the MAPK and PI3K pathways, upstream kinases Raf, MEK, and PI3K have one primary substrate, while downstream kinases ERK, AKT, and mTOR have multiple substrates. Mutations in PI3K/AKT/mTOR kinases are more abundant than mutations in MAPK kinases.
Ugi adduct 8 exhibited potent anti-cancer against NSCLC cancer cells though caspase-mediated apoptosis and PI3K/mTOR inhibition signaling pathway.
In this study, novel morpholinopyrimidine-5-carbonitriles were designed and synthesized as dual PI3K/mTOR inhibitors and apoptosis inducers.
A novel series of procaine derivatives incorporating 1,2,3-triazole and isoxazoline scaffolds were developed and evaluated for their anticancer potential, particularly against esophageal cancer.