29171-45-7Relevant academic research and scientific papers
INHIBITORS OF INTEGRATED STRESS RESPONSE PATHWAY
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, (2019/12/28)
The present disclosure relates generally to therapeutic agents that may be useful as inhibitors of Integrated Stress Response (ISR) pathway.
Discovery of carboranes as inducers of 20S proteasome activity
Ban, Hyun Seung,Minegishi, Hidemitsu,Shimizu, Kazuki,Maruyama, Minako,Yasui, Yuka,Nakamura, Hiroyuki
experimental part, p. 1236 - 1241 (2011/02/21)
(Chemical Equation Presented) The carborane framework gives analogues able to induce 20S proteasome activities. A series of ortho-carboranylphenoxy derivatives were synthesized as 20S proteasome agonists, and carborane derivatives 11 a and 11 b were found
Boron-containing phenoxyacetanilide derivatives as hypoxia-inducible factor (HIF)-1α inhibitors
Shimizu, Kazuki,Maruyama, Minako,Yasui, Yuka,Minegishi, Hidemitsu,Ban, Hyun Seung,Nakamura, Hiroyuki
scheme or table, p. 1453 - 1456 (2010/07/06)
A series of boron-containing phenoxyacetanilide derivatives 8a-f, 9a-f, 15, and 16 were synthesized as hypoxia-inducible factor (HIF)-1α inhibitors. Among the compounds synthesized, carboranylphenoxyacetanilide 16 (GN26361) was found to be a potent inhibitor against HIF-1α accumulation under hypoxic conditions and inhibited the hypoxia-induced HIF-1 transcriptional activity in HeLa cells (IC50 = 0.74 μM). Compound 16 suppressed hypoxia-induced HIF-1α accumulation and vascular endothelial growth factor mRNA expression in a concentration-dependent manner without affecting the expression of HIF-1α mRNA.
Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA1/GPR40), a potential target for the treatment of type II diabetes
Christiansen, Elisabeth,Urban, Christian,Merten, Nicole,Liebscher, Kathrin,Karlsen, Kasper K.,Hamacher, Alexandra,Spinrath, Andreas,Bond, Andrew D.,Drewke, Christel,Ullrich, Susanne,Kassack, Matthias U.,Kostenis, Evi,Ulven, Trond
scheme or table, p. 7061 - 7064 (2009/11/30)
A series of 4-phenethynyldihydrocinnamic acid agonists of the free fatty acid receptor 1 (FFA1) has been discovered and explored. The preferred compound 20 (TUG-424, EC50 = 32 nM) significantly increased glucose-stimulated insulin secretion at 100 nM and may serve to explore the role of FFA1 in metabolic diseases such as diabetes or obesity.
