216060-23-0Relevant articles and documents
KDM1A INHIBITORS FOR THE TREATMENT OF DISEASE
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Paragraph 0431; 0433, (2016/09/26)
Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.
Biarylcarboxybenzamide derivatives as potent vanilloid receptor (VR1) antagonistic ligands
Park, Hyeung-Geun,Choi, Ji-Yeon,Kim, Mi-Hyun,Choi, Sea-Hoon,Park, Mi-Kyung,Lee, Jihye,Suh, Young-Ger,Cho, Hawon,Oh, Uhtaek,Kim, Hee-Doo,Joo, Yung Hyup,Shin, Song Seok,Kim, Jin Kwan,Jeong, Yeon Su,Koh, Hyun-Ju,Park, Young-Ho,Jew, Sang-Sup
, p. 631 - 634 (2007/10/03)
Seventeen biarylcarboxybenzamide derivatives were prepared for the study of their agonistic/antagonistic activities to the vanilloid receptor (VR1) in rat DRG neurons. The replacement of the piperazine moiety of the lead compound 1 with phenyl ring showed quite enhanced antagonistic activity. Among the prepared derivatives, N-(4-tert-butylphenyl)-4-pyridine-2-yl-benzamide (2, IC 50 = 31 nM) and N-(4-tert-butylphenyl)-4-(3-methylpyridine-2-yl) benzamide (3g, IC50 = 31 nM), showed 5-fold higher antagonistic activity than 1 in 45Ca2+-influx assay.