Design and synthesis of chromene-1,2,3-triazole benzene sulfonamide hybrids as potent carbonic anhydrase-IX inhibitors against prostate cancer
Fawzia Faleh Albelwi, Mohamed S. Nafie, Nader R. Albujuq, Wafa Hourani, Ateyatallah Aljuhani, Khaled M. Darwish, Mohamed M. Tawfik, Nadjet Rezki, Mohamed Reda Aouad
Abstract
values of 0.113, 0.134, and 0.214 μM. The most active compound, 10a, was tested for apoptosis-induction; it induced apoptosis by 31.9-fold cell cycle arrest at the G1-phase. Further, the molecular modeling approach highlighted the relevant binding affinity for the top-active compound 10a against CA IX as one of the most prominent PC-3 prostate cancer-associated biotargets.
Topics & Concepts
SulfonamideProstate cancerCarbonic anhydraseTriazoleChemistryCarbonic anhydrase IIEnzymeBenzeneApoptosisCancer researchCancerPharmacologyCombinatorial chemistryBiochemistryStereochemistryMedicineInternal medicineOrganic chemistryEnzyme function and inhibitionSynthesis and Catalytic ReactionsCholinesterase and Neurodegenerative Diseases