339063-00-2Relevant academic research and scientific papers
New Pyrano-4H-benzo[g]chromene-5,10-diones with Antiparasitic and Antioxidant Activities
Al Nasr, Ibrahim S.,Jentzsch, Jana,Shaikh, Amin,Singh Shuveksh, Priti,Koko, Waleed S.,Khan, Tariq A.,Ahmed, Khursheed,Schobert, Rainer,Ersfeld, Klaus,Biersack, Bernhard
, (2021)
New pyranonaphthoquinone derivatives were synthesized and investigated for their activity against Trypanosoma brucei, Leishmania major, and Toxoplasma gondii parasites. The pentafluorophenyl derivative was efficacious against T. brucei with single digit m
Synthesis, in vitro and in silico screening of 2-amino-4-aryl-6-(phenylthio) pyridine-3,5-dicarbonitriles as novel α-glucosidase inhibitors
Ali, Muhammad,Faramarzi, Mohammad Ali,Jabbar, Abdul,Khan, Khalid Mohammed,Larijani, Bagher,Mahdavi, Mohammad,Perveen, Shahnaz,Salar, Uzma,Shamim, Shahbaz,Taha, Muhammad
, (2020/05/16)
Inhibition of α-glucosidase enzyme is of prime importance for the treatment of diabetes mellitus (DM). Apart of many organic scaffolds, pyridine based compounds have previously been reported for wide range of bioactivities. The current study reports a series of pyridine based synthetic analogues for their α-glucosidase inhibitory potential assessed by in vitro, kinetics and in silico studies. For this purpose, 2-amino-4-aryl-6-(phenylthio)pyridine-3,5-dicarbonitriles 1–28 were synthesized and subjected to in vitro screening. Several analogs, including 1–3, 7, 9, 11–14, and 16 showed many folds increased inhibitory potential in comparison to the standard acarbose (IC50 = 750 ± 10 μM). Interestingly, compound 7 (IC50 = 55.6 ± 0.3 μM) exhibited thirteen-folds greater inhibition strength than the standard acarbose. Kinetic studies on most potent molecule 7 revealed a competitive type inhibitory mechanism. In silico studies have been performed to examine the binding mode of ligand (compound 7) with the active site residues of α-glucosidase enzyme.
4, 6-diaryl pyran derivative and application thereof in preparation of liver cancer drugs
-
Paragraph 0034; 0036; 0037, (2017/07/23)
The invention relates to 4, 6-diaryl pyran derivative and application thereof in the preparation of liver cancer drugs. The 4, 6-diaryl pyran derivative as shown in general formula (I) and pharmaceutically acceptable salt, aquo-complex, solvate or optical isomer thereof have anti-tumor effect, and are particularly applied to the preparation of drugs for treating and/or preventing liver cancer. The compound has good antitumor drug development and application prospects.
