DERIVATIVES OF 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, PREPARATION AND THERAPEUTIC USE THEREOF AS HIF ACTIVATORS
申请人:ALTENBURGER Jean-Michel
公开号:US20110294788A1
公开(公告)日:2011-12-01
The present invention relates to novel substituted dihydropyrazolone derivatives, to their preparation and to their therapeutic use as activators of the transcription factor HIF.
Derivatives of 2-pyridin-2-yl-pyrazol-3(2H)-one, preparation and therapeutic use thereof as HIF activators
申请人:Altenburger Jean-Michel
公开号:US08541455B2
公开(公告)日:2013-09-24
The present invention relates to novel substituted dihydropyrazolone derivatives, to their preparation and to their therapeutic use as activators of the transcription factor HIF.
Inhibition of cancer cell invasion by new ((3,4-dihydroxy benzylidene)hydrazinyl)pyridine-3-sulfonamide analogs
作者:Seong-Mook Kang、Ky-Youb Nam、Seung-Youn Jung、Kyung-Hee Song、Seongho Kho、Kyoung Tai No、Hyun Kyung Choi、Jie-Young Song
DOI:10.1016/j.bmcl.2015.12.093
日期:2016.2
Rab GTPases regulate various types of intracellular membrane trafficking in all eukaryotes. Since Rab27a and its multiple effectors are involved in exocytosis of lysosome-related organelles and play a major role in malignancy, compounds targeting Rab27a could be likely used to inhibit invasive growth and tumor metastasis. Thus, we designed and synthesized several compounds based on the previously reported Rab27a-targeting synthetic compounds identified by virtual screening, and investigated their anti-metastatic effects in MDA-MB231 and A375 cells. Among the synthesized compounds, (E)-N-(3-chlorophenyl)-6-(2-(3,4-dihydroxy benzylidene)hydrazinyl)pyridine-3-sulfonamide (3d) and (E)-N-benzyl-6-(2-(3,4-dihydroxy benzylidene)hydrazinyl)-N-methylpyridine-3-sulfonamide (3f) significantly inhibited the invasiveness of both tumor cell lines. Compounds 3d and 3f also decreased the levels of signature extracellular matrix marker proteins (fibronectin, collagen, and a-smooth muscle actin) and representative mesenchymal cell markers (N-cadherin and vimentin). Taken together, our results suggest that novel sulfonamide analogs have anti-metastatic activity in breast and melanoma cancer cell lines and may be used as therapeutic agents to treat malignant cancer. (C) 2016 Elsevier Ltd. All rights reserved.
DERIVES DE 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE COMME ACTIVATEURS DE HIF
申请人:SANOFI
公开号:EP2382205A2
公开(公告)日:2011-11-02
DÉRIVÉS DE 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, LEUR PRÉPARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE COMME ACTIVATEURS DE HIF