Synthesis and Biological Evaluation of Novel 1, 5-Diarylpyrazole-3- carboxamide Compounds as Inhibitors of ALK5

Ten new 1, 5-diarylpyrazole-3-carboxamide compounds were synthesized and their structures were identified by 1H-NMR and FAB-MS. The primary biological tests showed that compound 4j exhibited some ALK5 inhibitory activity at concentration of 1μmol/L.

Synthesis and biological evaluation of novel 2,4,5-triaryl-1 H-pyrazol-3(2H)-ones as inhibitors of ALK5

一系列 2,4,5-triaryl 在 vitro 作为 ALK5 禁止者代替了 1H-pyrazol-3 (2H )-ones, ，是 desigened，综合并且评估。大多数混合物在 1 μ m ol/L 展出了显著 ALK5 抑制活动并且没在 30 μ m ol/L 显示重要 cytotoxicities。

Asymmetric Synthesis of (-)-(4R, 5R)-4-[5-(Benzo[1, 3]dioxol-5-yl)-4- hydroxyl-1-(pyridin-2-yl)-4, 5-dihydro-1H-pyrazol-3-yl]benzamide

The asymmetric synthesis of (-)-(4R, 5R)-4-[5-(benzo[1, 3]dioxol-5-yl)-4-hydroxyl-1- (pyridin-2-yl)-4,5-dihydro-1H-pyrazol-3-yl]-benzamide with improved Juliá-Colonna asymmetric epoxidation procedure as key step was described.