First-in-Class Star-Shaped Triazine Dendrimers Endowed with MMP-9 Inhibition and VEGF Suppression Capacity: Design, Synthesis, and Anticancer Evaluation
Nesreen S. Haiba, Hosam H. Khalil, Ahmed Bergas, Marwa M. Abu‐Serie, Sherine N. Khattab, Mohamed Teleb
Abstract
could possibly chelate the active site Zn of MMP-9 and form hydrogen-bonding interactions with the ligand essential backbone Tyr423. In addition, it suppressed the correlated oncogenic mediators VEGF and cyclin D, upregulated p21 expression, induced apoptosis (>75%), and inhibited the tumor cell migration (∼84%) in the treated cancer cells. Thus, up to our knowledge, it is the first triazine-based MMP-9 inhibitor dendrimer endowed with VEGF suppression potential that can be employed as a bioactive carrier.
Topics & Concepts
ChemistryMatrix metalloproteinaseDendrimerCytotoxicityHydrazideTriazineHydroxamic acidDocking (animal)Cancer cellCancer researchBiochemistryStereochemistryCancerBiologyIn vitroMedicineGeneticsNursingPolymer chemistryOrganic chemistryDendrimers and Hyperbranched PolymersRNA Interference and Gene DeliverySynthesis and Characterization of Heterocyclic Compounds