Synthesis and biological evaluation of 1,5-diphenylpyrrole derivatives as COX-2 selective inhibitors and NO-releasing agents and development of a novel BRD9 chemical probe
Sapienza Università Editrice, 30 giu 2020 - 128 pagine
This PhD thesis consists of three projects: the first and the second ones, carried out at Sapienza University of Rome, deal with the design and synthesis of novel COX-2 selective inhibitors and dual COX-2 inhibitors/NO-releasing agents, respectively. The third project concerns the development of a novel BRD9 chemical probe and was realized at the University of Oxford (Department of Chemistry).
1H NMR acetic acid activity added AGENTS AND DEVELOPMENT amide analysis assess binding biological evaluation BRD9 CHEMICAL PROBE broad cancer CDCl3 celecoxib cells characterized Chem Chemical structures chromatography concentration corresponding COX-2 selective inhibitors crude derivatives determined DMSO docking dried effects efficacy endowed ESI-mass ester et al ether ethyl expressed extracted Figure Finally function further give increase inhibition inhibitors and NO-releasing interaction ligand M+Na means mixture mmol moiety molecules MS-ESI needles NO-releasing agents NOVEL BRD9 CHEMICAL obtained organic phase oxide performed phenyl potency preparation presence pressure procedure properties proteins proved purified reaction reduced RELEASING AGENTS replacement reported respectively response ring RIVATIVES showed solubility solution stirred studies substituent suitable Synthesis Table temperature tested compounds tion values VELOPMENT vitro vivo washed White powder white solid writhes yield