Pegylated wortmannin and 17-hydroxywortmannin conjugates as phosphoinositide 3-kinase inhibitors active in human tumor xenograft models
T Zhu, J Gu, K Yu, J Lucas, P Cai, R Tsao… - Journal of medicinal …, 2006 - ACS Publications
T Zhu, J Gu, K Yu, J Lucas, P Cai, R Tsao, Y Gong, F Li, I Chaudhary, P Desai, M Ruppen…
Journal of medicinal chemistry, 2006•ACS PublicationsPhosphoinositide 3-kinase (PI3K) is an important target for cancer chemotherapy due to the
deregulation of its signaling pathway in a wide spectrum of human tumors. Wortmannin and
its analogues are potent PI3K inhibitors whose therapeutic use has been impeded by
inherent defects such as instability and toxicity. Pegylation of wortmannin and 17-
hydroxywortmannin gives rise to conjugates with improved properties, including a higher
therapeutic index. Pegylated 17-hydroxywortmannin (8, PWT-458) has been selected for …
deregulation of its signaling pathway in a wide spectrum of human tumors. Wortmannin and
its analogues are potent PI3K inhibitors whose therapeutic use has been impeded by
inherent defects such as instability and toxicity. Pegylation of wortmannin and 17-
hydroxywortmannin gives rise to conjugates with improved properties, including a higher
therapeutic index. Pegylated 17-hydroxywortmannin (8, PWT-458) has been selected for …
Phosphoinositide 3-kinase (PI3K) is an important target for cancer chemotherapy due to the deregulation of its signaling pathway in a wide spectrum of human tumors. Wortmannin and its analogues are potent PI3K inhibitors whose therapeutic use has been impeded by inherent defects such as instability and toxicity. Pegylation of wortmannin and 17-hydroxywortmannin gives rise to conjugates with improved properties, including a higher therapeutic index. Pegylated 17-hydroxywortmannin (8, PWT-458) has been selected for further development.
ACS Publications