70853-28-0Relevant academic research and scientific papers
COMPOUNDS THAT INHIBIT HIF-1 ACTIVITY, THE METHOD FOR PREPARATION THEREOF AND THE PHARMACEUTICAL COMPOSITION CONTAINING THEM AS AN EFFECTIVE COMPONENT
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Page/Page column 35, (2009/12/24)
Disclosed herein are an HIF-1 inhibitor, a method for the preparation thereof, and a pharmaceutical composition comprising the same as an active ingredient. The HIF-1 inhibitor shows anticancer activity thanks to the inhibition activity against HIF-1, a transcription factor which plays an important role in the growth and metastasis of cancer, but not to general cytotoxicity. Thus, the HIF-inhibitor and a pharmaceutically acceptable salt thereof can be used as a therapeutic for various cancers such as liver cancer; stomach cancer and breast cancer. Also, the compound having inhibition activity against HIF-1 is useful in the treatment of diabetic retinopathy and arthritis, which are aggravated by HIF-1-mediated VEGF expression.
COMPOUNDS TEAT INHIBIT HBF-I ACTIVITY, THE METHOD FOR PREPARATION THEREOF AND THE PHARMACEUTICAL COMPOSITION CONTAINING THEM AS AN EFFECTIVE COMPONENT
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Page/Page column 46, (2008/06/13)
Disclosed herein are an HIF-I inhibitor, a method for the preparation thereof, and a pharmaceutical composition comprising the same as an active ingredient The BDDF-I inhibitor shows anticancer activity thanks to the inhibition activity against HIF-I, a transcription factor which plays an important role in the growth and metastasis of cancer, but not to general cytotoxicity. Thus, the HIF-inhibitor and a pharmaceutically acceptable salt thereof can be used as a therapeutic for various cancers such as liver cancer, stomach cancer and breast cancer. Also, the compound having inhibition activity against HDDF-I is useful in the treatment of diabetic retinopathy and arthritis, which are aggravated by HEF-l-mediated VEGF expression.
(Aryloxyacetylamino)benzoic acid analogues: A new class of hypoxia-inducible factor-1 inhibitors
Lee, Kyeong,Lee, Jeong Hyung,Boovanahalli, Shanthaveerappa K.,Jin, Yinglan,Lee, Mijeoung,Jin, Xuejun,Kim, Jin Hwan,Hong, Young-Soo,Lee, Jung Joon
, p. 1675 - 1684 (2008/02/01)
Structural modification of a compound discovered during screening using an HRE-dependent reporter assay has revealed a novel class of HIF-1 inhibitors, which potently inhibit the HIF-1α protein accumulation and its target gene expression under hypoxic conditions in human hepatocellular carcinoma Hep3B cells.
Identification of anthranilic acid derivatives as a novel class of allosteric inhibitors of hepatitis C NS5B polymerase
Nittoli, Thomas,Curran, Kevin,Insaf, Shabana,DiGrandi, Martin,Orlowski, Mark,Chopra, Rajiv,Agarwal, Atul,Howe, Anita Y. M.,Prashad, Amar,Floyd, M. Brawner,Johnson, Bernard,Sutherland, Alan,Wheless, Karen,Feld, Boris,O'Connell, John,Mansour, Tarek S.,Bloom, Jonathan
, p. 2108 - 2116 (2008/02/06)
A series of potent anthranilic acid-based inhibitors of the hepatitis C NS5B polymerase has been identified. The inhibitors bind to a site on NS5B between the thumb and palm regions adjacent to the active site as determined by X-ray crystallography of the enzyme-inhibitor complex. Guided by both molecular modeling and traditional SAR, the enzyme activity of the initial hit was improved by approximately 100-fold, yielding a series of potent and selective NS5B inhibitors with IC50 values as low as 10 nM. These compounds were also inhibitors of the HCV replicon in cultured HUH7 cells.
Acetylamino benzoic acid compounds and their use for nonsense suppression and the treatment of disease
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Page/Page column 13, (2008/06/13)
Novel acetylamino benzoic acid compounds, methods of using and pharmaceutical compositions comprising an acetylamino benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premat
Cloxacepride and related compounds: A new series of orally active antiallergic compounds
Metz,Pindell,Chen
, p. 1065 - 1070 (2007/10/02)
4-[(p-Chlorophenoxy)acetyllamino]-5-chloro-2-methoxy-N-[2-(diethylamino)ethyl]benzamide (cloxacepride) exhibited substantial oral antiallergic potential in a reaginic PCA test in rats over a wide range of antigenic challenge times. Available reference compounds with oral activity, such as doxantrazole and 7-(2-hydroxyethoxy)-9-oxo-xanthene-2-carboxylic acid (AH 7725, 4) were active only when administered 15 min before challenge: 4, in particular, was not consistent in effect. Oral ED50 values for cloxacepride of 46-49 mg/kg were comparable to that of theophylline and to an intravenous injection of 2 mg/kg of disodium chromoglycate (DSCG) followed by immediate challenge. Following oral ED50 doses, 1 showed slower onset and longer duration of action than theophylline. The absence of inhibition of systemic anaphylaxis and of antihistaminic activity suggests specific effect for reaginic antigen antibody reactions. Structure-activity relationships of various chemical modifications were investigated and discussed in terms of essential substituents.
