Novel pyrazolo[3,4-<i>d</i>]pyrimidine derivatives: design, synthesis, anticancer evaluation, VEGFR-2 inhibition, and antiangiogenic activity
Ahmed M. Abdelhamed, Rasha A. Hassan, Hanan H. Kadry, Amira A. Helwa
Abstract
= 0.035 ± 0.012 μM. Moreover, there was an excellent reduction in HUVEC migratory potential that resulted in a significant disruption of wound healing patterns by 23% after 72 h of treatment with compound 12b. Cell cycle and apoptosis investigations showed that compound 12b could stop the cell cycle at the S phase and significantly increase total apoptosis in the MDA-MB-468 cell line by 18.98-fold compared to the control. Moreover, compound 12b increased the caspase-3 level in the MDA-MB-468 cell line by 7.32-fold as compared to the control.
Topics & Concepts
StaurosporineApoptosisCell cycleIC50ChemistryCell cultureSunitinibPyrimidineCell cycle checkpointPharmacologyCell growthStereochemistryIn vitroKinaseBiochemistryCancerBiologyMedicineInternal medicineProtein kinase CGeneticsSynthesis and biological activityMulticomponent Synthesis of HeterocyclesQuinazolinone synthesis and applications