This study developed novel progesterone-based CDK8 inhibitors and demonstrated their anticancer activity against A549 cells in CS-PEG nanoform, supported by gene expression analysis, CDK8 inhibition, and molecular docking studies.
Compound 19 arrested the MCF-7 cells at the G2/M phase probably through inhibition of CDK1 and elicited apoptosis. It did not violate Lipinski's rule of five and has a low blood brain barrier penetration and high intestinal absorption.
Design and synthesis a novel of 2-oxo-pyridine and 1′H-spiro-pyridine derivatives as a new apoptotic inducers agents.
New thiopyrimidine/chalcone hybrids were synthesized for hepatocellular carcinoma treatment. Compound 5h was the most active one. Additionally, it displayed STAT3/STAT5 dual inhibitory action which was confirmed by western blot analysis.
Two pyrimidine hybrid series (6a–g, 10a–d) were synthesized. Compounds 6c and 10b showed anti-proliferative activity against MCF-7, strong EGFR-TK inhibition, and docking confirmed effective binding. In silico studies suggest safe, orally bioavailable candidates.