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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Zask, A. et al.

Arie Zask, Joshua Kaplan, Lourdes Toral-Barza, Irwin Hollander, Mairead Young, Mark Tischler, Christine Gaydos, Michael Cinque, Judy Lucas, Ker Yu,

Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy.

The phosphoinositide 3-kinase (PI3K) signaling pathway is frequently up-regulated in human cancer and is a promising target for the treatment of cancer. Wortmannin and its analogues are potent inhibitors of PI3K but suffer from inherent defects such as instability, insolubility, and toxicity. Opening of the reactive furan ring of 17-hydroxywortmannin with amines gives compounds with improved properties such as greater stability and aqueous solubility and a larger therapeutic index. Ring-opened analogues such as compound 13 containing basic amine groups have significantly increased PI3K inhibitory potency and greater efficacy in nude mouse xenograft assays.[1]

References

Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy. Zask, A., Kaplan, J., Toral-Barza, L., Hollander, I., Young, M., Tischler, M., Gaydos, C., Cinque, M., Lucas, J., Yu, K. J. Med. Chem. (2008) [Pubmed]

Annotations and hyperlinks in this abstract are from individual authors of WikiGenes or automatically generated by the WikiGenes Data Mining Engine. The abstract is from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.About WikiGenes Open Access Licence Privacy Policy Terms of Use apsburg