New pyrazolo[3,4- <i>d</i> ]pyrimidine derivatives as EGFR-TK inhibitors: design, green synthesis, potential anti-proliferative activity and P-glycoprotein inhibition
Aya I. Hassaballah, Asmaa M. AboulMagd, Magdy M. Hemdan, Mohamed H. Hekal, Amira A. El‐Sayed, Paula S. Farag
Abstract
= 0.267 and 0.844 μM, respectively. Additionally, compound 16 was found to induce cell cycle arrest at the S phase with a subsequent increase in pre-G cell population in MDA-MB-468 cell line. It also increased the percentage of apoptotic cells in a time-dependent manner. Moreover, a molecular docking study was carried out to explain the target compounds' potent inhibitory activity within the EGFR binding site.
Topics & Concepts
PyrimidineChemistryCytotoxicityIC50Cell cycleCell cycle checkpointCell cultureStereochemistryCell growthApoptosisDocking (animal)PopulationCytotoxic T cellBiochemistryIn vitroBiologyMedicineNursingGeneticsEnvironmental healthSynthesis and biological activityMulticomponent Synthesis of HeterocyclesSynthesis and Characterization of Heterocyclic Compounds