Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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Development of Novel Small Chemical Inhibitors for Lck SH Domain with in vitro T-cell Inhibitory Activity

  • Published : 2006.09.20
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Abstract

We investigated in vitro T-cell inhibitory activity and bioavailability of small chemical inhibitors for Lck SH2 domain, which had a different scaffold such as an amide bond, reduced amide bond, N-methyl amide bond, thioamide bond, and urethane bond. Each of these compounds, with its particular scaffold, showed a different logP value, stability against serum enzyme, stability in buffer solution, and in vitro T-cell inhibitory activity. Overall results indicated that the SH2 inhibitor containing urethane bond can be a new lead compound because of its superior bioavailability, potent in vitro T-cell inhibitory activity, and facile synthesis.

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Cited by

  1. Development of Novel Small Chemical Inhibitors for Lck SH Domain with in vitro T-Cell Inhibitory Activity. vol.38, pp.7, 2007, https://doi.org/10.1002/chin.200707217