유경호 김세영 류재천 2024-01-20T22:35:31Z 2024-01-20T22:35:31Z 2021-09-06 2008-09 1225-9098 https://pubs.kist.re.kr/handle/201004/133177 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 IC50 value of 620 μM 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-l were synthesized and evaluated for Akt1 inhibitory activity. Korean 한국응용과학기술학회 1,3,4-Thiadiazole 유도체의 합성 및 Akt1 카이네이즈 저해 활성 Synthesis and Akt1 Kinase Inhibitory Activity of 1,3,4-Thiadiazole Derivatives Article 2 한국응용과학기술학회지, v.25, no.3, pp.370 - 379 한국응용과학기술학회지 25 3 370 379 kci ART001279159 1 3 4-thiadiazoles synthesis Akt1 kinase inhibitory activity