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J Med Chem. 2006 Feb 23;49(4):1373-8.

Pegylated wortmannin and 17-hydroxywortmannin conjugates as phosphoinositide 3-kinase inhibitors active in human tumor xenograft models.

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1
Preclinical Development, Wyeth Research, 401 North Middletown Road, Pearl River, New York 10965, USA.

Abstract

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.

PMID:
16480272
DOI:
10.1021/jm050901o
[Indexed for MEDLINE]

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