公开(公告)号：US20070207992A1

公开(公告)日：2007-09-06

申请号：US11708226

申请日：2007-02-20

申请人： David Wenkert ,  Leslie Kuhn ,  Erica Scheller ,  Michael Kron ,  Yuehai Shen

发明人： David Wenkert ,  Leslie Kuhn ,  Erica Scheller ,  Michael Kron ,  Yuehai Shen

IPC分类号： A61K31/397 ,  C07D403/02

CPC分类号： C07D225/06

摘要： The present invention relates to novel geldanamycin derivatives which have antitumor and antiparasitic properties. The geldanamycin derivatives disclosed herein have antitumor properties in humans due to their interaction with human heat shock protein 90 (hsp90). The human parasites Plasmodium falciparum, Trypanosoma Cruzi, and Leishmania donovani are lethally susceptible to exposure to geldanamycin via complexation of geldanamycin with their homologs (Pfhsp90, hsp83, and hsp90, respectively) of the human hsp90. The geldanamycin derivatives disclosed herein also interact with these parasitic hsp90 homologs so as to have antiparasitic properties.

摘要翻译： 本发明涉及具有抗肿瘤和抗寄生虫性质的新型格尔德霉素衍生物。 本文公开的格尔德霉素衍生物由于与人类热休克蛋白90（hsp90）的相互作用而在人体中具有抗肿瘤特性。 人类寄生虫恶性疟原虫，克氏锥虫和杜氏利什曼原虫通过与人类hsp90的同源物（分别为Pfhsp90，hsp83和hsp90）的复合而容易接触格尔德霉素。 本文公开的格尔德霉素衍生物还与这些寄生的hsp90同源物相互作用以具有抗寄生虫性质。