公开(公告)号：US20060041010A1

公开(公告)日：2006-02-23

申请号：US10921332

申请日：2004-08-19

申请人： Tak-Hang Chan ,  Wai-Har Lam ,  Larry Chow ,  Qing Dou ,  Deborah Kuhn ,  Aslamuzzaman Kazi

发明人： Tak-Hang Chan ,  Wai-Har Lam ,  Larry Chow ,  Qing Dou ,  Deborah Kuhn ,  Aslamuzzaman Kazi

IPC分类号： A61K31/353 ,  C07D311/22

CPC分类号： C07D311/62 ,  Y02P20/582

摘要： (−)-EGCG, the most abundant catechin, was found to be chemopreventive and anticancer agent. However, (−)-EGCG has at least one limitation: it gives poor bioavailability. This invention provides compounds of generally formula 10, wherein R1 is selected from the group of —H and C1 to C6 acyl group; R2, R3, and R4 are each independently selected from the group of —H, —OH, and C1 to C6 acyloxyl group; and at least one of R2, R3, or R4 is —H. The derivatives of (−)-EGCG that is at least as potent as (−)-EGCG. The carboxylate protected forms of (−)-EGCG and its derivatives are found to be more stable than the unprotected forms, which can be used as proteasome inhibitors to reduce tumor cell growth.

摘要翻译： （ - ） - EGCG是最丰富的儿茶素，被发现是化学预防和抗癌剂。 然而，（ - ） - EGCG至少有一个限制：它具有差的生物利用度。 本发明提供通式为10的化合物，其中R 1选自-H和C 1至C 6酰基基团; R 2，R 3和R 4各自独立地选自-H，-OH和C 1的基团 C 6 -C 5酰氧基; 并且R 2，R 3或R 4中的至少一个为-H。 （ - ） - EGCG的衍生物至少与（ - ） - EGCG一样有效。 发现羧酸酯保护形式的（ - ） - EGCG及其衍生物比未保护形式更稳定，可用作蛋白酶体抑制剂以减少肿瘤细胞生长。