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Journal of the Korean Chemical Society (JKCS)

ISSN 1017-2548(Print)
ISSN 2234-8530(Online)
Volume 55, Number 5
JKCSEZ 55(5)
October 20, 2011 

Design, Synthesis and Biological Evaluation of Novel Analogs of Bortezomib
R Janaki Rama Rao, A K S Bhujanga Rao*, K Swapna, B Baby Rani, S Prasanna Kumar, S Awantika, Y L N Murthy
Bortezomib, human tumor cell lines, A549, PC3, IC50 values
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 IC50 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 IC50 values of bortezomib in these cell lines are 27.3 nM and 42.0 nM.
765 - 772
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