Journal of the Korean Applied Science and Technology (한국응용과학기술학회지)

The Korean Society of Applied Science and Technology (한국응용과학기술학회)
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Synthesis and Akt1 Kinase Inhibitory Activity of 1,3,4-Thiadiazole Derivatives

1,3,4-Thiadiazole 유도체의 합성 및 Akt1 카이네이즈 저해 활성

  • 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)
  • 유경호 (한국과학기술연구원 생체과학연구본부) ;
  • 김세영 (한국과학기술연구원 생체과학연구본부) ;
  • 류재천 (한국과학기술연구원 생체과학연구본부)
  • Published : 2008.09.30
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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.

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