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http://dx.doi.org/10.12925/jkocs.2008.25.3.13

Synthesis and Akt1 Kinase Inhibitory Activity of 1,3,4-Thiadiazole Derivatives  

Yoo, Kyung-Ho (Life Sciences Research Division, Korea Institute of Science and Technology)
Kim, Se-Young (Life Sciences Research Division, Korea Institute of Science and Technology)
Ryu, Jae-Chun (Life Sciences Research Division, Korea Institute of Science and Technology)
Publication Information
Journal of the Korean Applied Science and Technology / v.25, no.3, 2008 , pp. 370-379 More about this Journal
Abstract
Akt, a serine/threonine protein kinase as a viral oncogene, is a critical regulator of PI3K-mediated cell proliferation and survival. On translocation, Akt is phosphorylated and activated, ultimately resulting in stimulation of cell growth and survival. As a part of our program toward the novel Akt1 inhibitors with potent activity over PI3K signaling pathway, we found primary hit compound 2 with an $IC_{50}$ value of $620\mu}M$ from protein kinase focused library. Based on the structural features of 2, new 1,3,4-thiadiazole derivatives were designed by the introduction of aromatic and heteroaromatic moieties onto thiadiazole nucleus. In this work, a series of 1,3,4-thiadiazole derivatives 1a-1 were synthesized and evaluated for Akt1 inhibitory activity.
Keywords
1,3,4-thiadiazoles; synthesis; Akt1 kinase; inhibitory activity;
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