Bioorganic and Medicinal Chemistry Letters p. 1680 - 1683 (2013)
Update date:2022-08-04
Topics:
Akama, Tsutomu
Virtucio, Charlotte
Dong, Chen
Kimura, Richard
Zhang, Yong-Kang
Nieman, James A.
Sharma, Rashmi
Lu, Xiaosong
Sales, Marcelo
Singh, Rajeshwar
Wu, Anne
Fan, Xiao-Qing
Liu, Liang
Plattner, Jacob J.
Jarnagin, Kurt
Freund, Yvonne R.
A series of novel 6-(aminomethylphenoxy)benzoxaborole analogs was synthesized for the investigation of the structure-activity relationship of the inhibition of TNF-alpha, IL-1beta, and IL-6, from lipopolysaccharide stimulated peripheral blood mononuclear cells. Compounds 9d and 9e showed potent activity against all three cytokines with IC50 values between 33 and 83 nM. Chloro substituted analog 9e (AN3485) is considered to be a promising lead for novel anti-inflammatory agent with a favorable pharmacokinetic profile.
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Doi:10.1111/cbdd.12091
(2013)Doi:10.1016/j.ejmech.2012.12.023
(2013)Doi:10.1002/kin.20759
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(2014)
