甾体 C-21 杂芳基硫醚。第 3 部分：孕-4-烯-[3,2-c]吡唑并 A 环修饰的甾体作为选择性糖皮质激素受体调节剂（分离的甾体）。
Steroidal C-21 heteroaryl thioethers. Part 3: pregn-4-eno-[3,2-c]pyrazole fused A ring modified steroids as selective glucocorticoid receptor modulators (dissociated steroids).
机构信息
Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
出版信息
Bioorg Med Chem Lett. 2012 May 1;22(9):3291-5. doi: 10.1016/j.bmcl.2012.03.015. Epub 2012 Mar 11.
The introduction of A ring pyrazole modification to the hydrocortisone C-21 heteroaryl thioethers generated compounds with excellent transrepression potency (IL-8 inhibition) compared to their hydrocortisone analogs. However, the transcriptional transactivation activity of these compounds were considerably higher than the corresponding hydrocortisone analogs. Among all the compounds evaluated, a quinoxaline thioether modification demonstrated the best overall in vitro separation.
将 A 环吡唑修饰引入到氢化可的松 C-21 杂芳基硫醚中，与氢化可的松类似物相比，生成的化合物具有优异的反式抑制作用（IL-8 抑制）。然而，这些化合物的转录反式激活活性明显高于相应的氢化可的松类似物。在所评估的所有化合物中，喹喔啉硫醚修饰表现出最佳的整体体外分离。
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