Design, synthesis, and biological evaluation of 2, 4-dichlorophenoxyacetamide chalcone hybrids as potential c-Met kinase inhibitors
Abstractc-Met is involved in cellular processes that lead to the development and progression of cancer. A series of 2, 4-dichlorophenoxyacetamide-chalcones were synthesized and evaluated for their antiproliferative activities against MCF-7, HT-29, and A549 cancer cell lines. Several compounds showed moderate-to-good antiproliferative activity against MCF-7 and A549 cell lines. Many compounds were inactive against the HT-29 cell line. Some selected compounds were tested against c-Met kinase using the ADP GloTM assay and were found to possess IC50 < 10 µM indicating good activity. Compound6f was identified as a pr...
Source: Medicinal Chemistry Research - November 24, 2022 Category: Chemistry Source Type: research
Design, synthesis and anticancer activity studies of novel indole derivatives as Bcl-2/Mcl-1 dual inhibitors
AbstractA series of novel indole derivatives were designed, synthesized and evaluated for the binding affinity of Bcl-2 family proteins and antiproliferative activity against three selected cancer cell lines (PC-3, Jurkat, and MDA-MB-231). The preliminary structure-activity relationship (SAR) for this indole scaffold was summarized. Among all the compounds, compound9k showed the best inhibitory activity against Bcl-2 and Mcl-1 proteins with IC50 values of 7.63 µM and 1.53 µM, respectively, which is comparable to the positive control AT-101. The docking study of it with Bcl-2 and Mcl-1 proteins indicated that it coul...
Source: Medicinal Chemistry Research - November 18, 2022 Category: Chemistry Source Type: research
Synthesis, antimicrobial, and antioxidant activities of disubstituted 1,2,3-triazoles with amide-hydroxyl functionality
AbstractA series of 1,4-disubstituted 1,2,3-triazoles with amide-hydroxyl functionality(5a –5t) was synthesized from aliphatic alkynes(4a –4e) and aromatic bromides(3a –3d) in presence of catalytic amount of cellulose CuI nanoparticles. All the synthesized triazoles were characterized by various analytical techniques: FTIR,1H NMR,13C NMR and HRMS. Further, all the synthesized compounds were screened for in vitro antioxidant and antimicrobial activities. The antioxidant activity of the compound5s was found better than other compounds. Compounds5h and5l exhibited good antibacterial and antifungal activity, respectively...
Source: Medicinal Chemistry Research - November 17, 2022 Category: Chemistry Source Type: research
Synthesis of myricetin derivatives and evaluation of their hypoglycemic activities
AbstractMyricetin is a common plant-derived flavonoid and exhibits a wide range of activities. However, myricetin also exhibits substantial limitations, such as its poor water-solubility and low stability in body when it was administrated orally. To solve these problems, a series of myricetin derivatives with different disaccharide groups were designed, synthesized and evaluated their hypoglycemic activities. All synthesized compounds displayed significant α-glucosidase inhibitory activity in comparison with acarbose in vitro, which indicated that myricetin derivatives with different disaccharide groups had good hypoglyce...
Source: Medicinal Chemistry Research - November 10, 2022 Category: Chemistry Source Type: research
A study from structural insight to the antiamyloidogenic and antioxidant activities of flavonoids: scaffold for future therapeutics of Alzheimer ’s disease
AbstractNeurotoxicity occurs in Alzheimer ’s disease due to the formation of Amyloid-β peptide aggregates and damage caused by oxidative stress. Upon aggregation of amyloid-β peptides, oxidative stress is generated; however, oxidative stress can also promote excess amyloid-β peptide production and aggregate formation. Currently availab le therapeutic options are little effective against Alzheimer’s disease, and they cannot stop the progression of the disease. As a new therapeutic alternative rather than inhibiting amyloid-β peptide production, inhibiting amyloid-β peptide aggregation along with oxidative stress ma...
Source: Medicinal Chemistry Research - November 9, 2022 Category: Chemistry Source Type: research
