当前位置: X-MOL 学术Bioorg. Med. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Identification of 1,6-dihydropyrazolo[4,3-c]carbazoles and 3,6-dihydropyrazolo[3,4-c]carbazoles as new Pim kinase inhibitors
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2013-05-16 , DOI: 10.1016/j.bmc.2013.05.011
Virginie Suchaud , Laurent Gavara , Emmanuelle Saugues , Lionel Nauton , Vincent Théry , Fabrice Anizon , Pascale Moreau

New 1,6-dihydropyrazolo[4,3-c]carbazoles and 3,6-dihydropyrazolo[3,4-c]carbazoles were prepared and evaluated for their Pim kinase inhibitory potencies as well as their antiproliferative activities toward two prostatic cancer cell lines. Pyrazolocarbazole 15a was found to be a potent Pim kinase modulator with inhibitory potency toward the three isoforms. Compound 6c strongly inhibited Pim-3 with weaker effect toward Pim-1 and Pim-2, and thus could be used as an interesting molecular tool to study Pim-3 biological functions.



中文翻译:

鉴定1,6-二氢吡唑并[4,3- c ]咔唑和3,6-二氢吡唑并[3,4- c ]咔唑作为新的Pim激酶抑制剂

制备了新的1,6-二氢吡唑并[4,3- c ]咔唑和3,6-二氢吡唑并[3,4- c ]咔唑,并评估了它们对Pim激酶的抑制能力以及对两种前列腺癌细胞系的抗增殖活性。 。发现吡唑并咔唑15a是有效的Pim激酶调节剂,对三种同工型具有抑制作用。化合物6c强烈抑制Pim-3,对Pim-1和Pim-2的作用较弱,因此可以用作研究Pim-3生物学功能的有趣分子工具。

更新日期:2013-05-16
down
wechat
bug