在C-8a位具有乙炔基且在A环和C环中含有氰基烯酮的新型三环化合物：高效抗炎和细胞保护剂。
Novel tricyclic compounds having acetylene groups at C-8a and cyano enones in rings A and C: highly potent anti-inflammatory and cytoprotective agents.
作者信息
Honda Tadashi, Sundararajan Chitra, Yoshizawa Hidenori, Su Xiaobo, Honda Yukiko, Liby Karen T, Sporn Michael B, Gribble Gordon W
机构信息
Department of Chemistry, Dartmouth College, 6128 Burke Laboratory, Hanover, New Hampshire 03755, USA.
出版信息
J Med Chem. 2007 Apr 19;50(8):1731-4. doi: 10.1021/jm070141c. Epub 2007 Mar 17.
Abstract
Novel C-8a functionalized tricyclic compounds having cyano enones in rings A and C have been synthesized and biologically evaluated. Among them, compounds with acetylene groups at C-8a show extremely high potency in in vitro and in vivo bioassays for anti-inflammatory and cytoprotective activities. Both in vitro and in vivo potencies are markedly higher than those of 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid (CDDO), which is being evaluated as an anticancer drug in phase I clinical trials.
摘要
已合成并对在A环和C环中具有氰基烯酮的新型C-8a官能化三环化合物进行了生物学评估。其中，在C-8a处带有乙炔基的化合物在抗炎和细胞保护活性的体外和体内生物测定中显示出极高的效力。体外和体内效力均明显高于正在进行I期临床试验评估的抗癌药物2-氰基-3,12-二氧代齐墩果-1,9(11)-二烯-28-酸（CDDO）。
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