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Synthesis and Antibacterial Activity of Novel 5-(heteroaryl)isoxazole Derivatives
RamaRao, R. Janaki,Rao, A.K.S. Bhujanga,Sreenivas, N.,Kumar, B. Suneel,Murthy, Y. L. N. Korean Chemical Society 2011 대한화학회지 Vol.55 No.2
Isoxazole계 화합물을 합성하고 항균활성연구를 수행하였다. 3-Di(alkylamino)acryloalkanones을 hydroxylamine hydrochloride 또는 hydroxylamine-O-sulphonic acid와 반응시켜서 target isoxazole계 화합물을 합성하였다. The synthesis, characterization and antibacterial activity of novel isoxazole derivatives were reported. 3-Di (alkylamino)acryloalkanones were prepared and used as synthons to get the target isoxazole derivatives via reaction with hydroxylamine hydrochloride or hydroxylamine-O-sulphonic acid.
Design, Synthesis and Biological Evaluation of Novel Analogs of Bortezomib
Rao, R. Janaki Rama,Rao, A.K.S. Bhujanga,Swapna, K.,Rani, B. Baby,Kumar, S. Prasanna,Awantika, S.,Murthy, Y.L.N. Korean Chemical Society 2011 대한화학회지 Vol.55 No.5
Novel analogs of bortezomib were designed, synthesized and in vitro biological evaluation was carried out using human tumor cell lines A549 and PC3. Docking studies of these analogs of bortezomib was discussed. According to biological investigations, the inhibitors 4, 6, and 8 were found to be more potent than reference drug candidate bortezomib. A549 cell line showed significant sensitivity towards 4, 6, and 8 with $IC_{50}$ values 14.03, 18.5, and 12.4 nM, respectively, and PC3 cell line showed IC50 values 26.1, 37.0, and 21.2 nM, respectively. The $IC_{50}$ values of bortezomib in these cell lines are 27.3 nM and 42.0 nM.