Design, synthesis and RNase A inhibition activity of catechin and epicatechin and nucleobase chimeric molecules.
Several novel catechin/epicatechin and nucleobase chimeric molecules 1-6 have been synthesized via azide-alkyne click chemistry. The structures of these hybrids have been confirmed by NMR and mass spectroscopic data. The synthesized molecules were tested for their RNase A inhibition activities. Gel-based assays showed inhibition in micromolar concentrations. The extent of inhibition was found to be dependent upon the nature of base as well as the configuration at C-3 position of catechin.
Roy
Basab
B
Department of Chemistry, Indian Institute of Technology, Kharagpur 721302, India.
Dutta
Sansa
S
Choudhary
Anupma
A
Chowdhary
Anupma
A
Basak
Amit
A
Dasgupta
Swagata
S
D000225:Adenine / Q000737:chemistry; D020134:Catalytic Domain; D002392:Catechin / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry / Q000379:methods; D008956:Models, Chemical; D009690:Nucleic Acid Conformation; D012259:Ribonuclease, Pancreatic / Q000037:antagonists & inhibitors*; D013696:Temperature
D002392:Catechin; D012259:Ribonuclease, Pancreatic; D000225:Adenine