54233-11-3Relevant academic research and scientific papers
Synthesis and biological evaluation of some amino- and sulfanyl-3H-quinazolin-4-one derivatives as potential anticancer agents
Malinowski, Zbigniew,Fornal, Emilia,Nowak, Monika,Kontek, Renata,Gajek, Gabriela,Borek, Bartlomiej
, p. 1723 - 1731 (2015)
A series of 6-substituted quinazolinone derivatives were prepared by the reaction of 6-bromoquinazolinones with aryl or alkyl amines and thiols, in the presence of a Pd(OAc)2/Xantphos system, under Buchwald-Hartwig-type reaction conditions. The 6-bromoquinazolinones were obtained in the three-components reaction of 5-bromoisatoic anhydride, triethyl orthoformate and an appropriate amine. Biological screening of the potential cytotoxicity of synthesized compounds on HT29 and HCT116 cell lines, as well as on the lymphocytes, showed that some derivatives of quinazolinone have significant anticancer activities. The detailed synthesis, spectroscopic data, and biological assays were reported.
Fragment-based discovery of hepatitis C virus NS5b RNA polymerase inhibitors
Antonysamy, Stephen S.,Aubol, Brandon,Blaney, Jeff,Browner, Michelle F.,Giannetti, Anthony M.,Harris, Seth F.,Hebert, Normand,Hendle, Joerg,Hopkins, Stephanie,Jefferson, Elizabeth,Kissinger, Charles,Leveque, Vincent,Marciano, David,McGee, Ethel,Najera, Isabel,Nolan, Brian,Tomimoto, Masaki,Torres, Eduardo,Wright, Tobi
, p. 2990 - 2995 (2008/12/23)
Non-nucleoside inhibitors of HCV NS5b RNA polymerase were discovered by a fragment-based lead discovery approach, beginning with crystallographic fragment screening. The NS5b binding affinity and biochemical activity of fragment hits and inhibitors was de
