期刊
CHEMICO-BIOLOGICAL INTERACTIONS
卷 246, 期 -, 页码 69-76出版社
ELSEVIER IRELAND LTD
DOI: 10.1016/j.cbi.2016.01.010
关键词
Derivatives of N-Chloro beta-lactams; Benzisoxazole derivatives; NF-kappa B inhibition; HDAC inhibition; In-silico studies
资金
- DST-SERB-FAST TRACK SCHEME [SR/FT/CS-93/2011]
- DST-SERB, Govt. of India [DST/SR/S1/OC-55/2012]
Novel N-chloro a-Lactam and benzisoxazole derivatives were successfully synthesized with excellent yields (92-96%) under simple and mild reaction conditions. The beta-lactams as a class acquired importance since the discovery of penicillin which contains beta-lactam unit as an essential structural feature of its molecule, this interest continued unabated because of the therapeutic importance of beta-lactam antibiotics. In silico studies of the compounds with cancer drug target enzymes showed the inhibition of HDAC (Histone Deacetylase) and NF-kappa B (nuclear factor kappa-light-chain-enhancer of activated B cells) significantly. The compounds were then investigated for the inhibitory potential against the same enzymes in vitro. NF-kappa B inhibition was investigated by trans activation assay using HEK293/NF-kappa B-luc cells. Overall, the synthesized compounds induce the cancer cell toxicity by restraining the NF-kappa B transcription factor mediated by HDAC inhibition and thus the compounds act as dual inhibitors. (C) 2016 Elsevier Ireland Ltd. All rights reserved.
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