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Glycosylated Polyamines As Anticancer, And Cancer Chemotherapeutic Compounds

技術優勢: In screening assays conducted by the Natinal Cancer Institute, one of the compounds has been shown to be more potent than tamoxifen in inhibiting growth of certain cancer cell lines.A detailed drug development plan is available for this technology.Stereochemically pure product is easily isolated and crystallized as a hydrochloride salt.

技術應用: These compounds can be used as anticancer, and chemotherapeutic agents against breast, ovarian, and a variety of other cancers. Based on the crystallographic studies of the structure of one of the compounds, these compounds are predicted to interact with the estrogen receptor, and thus can be used to modulate estrogen receptor activity in a variety of conditions or diseases involving estrogen-mediatedactivities including: (1) prevention or delay of the onset of breast cancer,(2) treatment or prevention of osteoporosis, (3) treatment, prevention or delaying of the onset of uterine disorders, (4) as a modulator of ovulation for purposes of fertility treatment and/or contaception, and (5) for reducing cardiovascular disease in postmenupausal women. Can be used as ligands in preparing metal complexes for developing analytical methodology.

*Abstract: Glycosylated polyamines comprising of mono- or oligo-saccharides that are glycosidically linked to an aliphatic polyamine, their pharmaceutically acceptable salts, prodrugs and derivatives are useful, for example, as anticancer compounds, and for the treatment of a variety of cancers. Methods for synthesis of glycosylated polyamines are disclosed. In addition, metal complexes of glycosylated polyamines, the preparation of such metal complexes and analytical methods using the metal complexes are provided. Methods for detecting equitorial and axial conformation of a group other than hydrogen at the C2 position of a saccharide molecule are also provided.

Also see:

S.P. Gaucher, S.P. Peterson, and J.A. Leary, Stereospecific Synthesis and Characterization of Amino Glycoside Ligands from Diethylenetriamine, J.Org.Chem., 1999 May 28: 64(11): 4012-15.

*Principal Investigation: Name: Sara Gaucher
Department:

Name: Julie Leary
Department:

Name: Steven Pedersen
Department:

附加資料: Patent Number: US6420344B1
Application Number: US2000524729A
Inventor: Leary, Julie A. | Gaucher, Sara P. | Pedersen, Steven F.
Priority Date: 16 Mar 1999
Priority Number: US6420344B1
Application Date: 14 Mar 2000
Publication Date: 16 Jul 2002
IPC Current: C07H001512 | C07H001526
US Class: 514042 | 514053 | 5360172 | 5360179 | 5360291
Assignee Applicant: The Regents of the University of California
Title: Glycosylated polyamines
Usefulness: Glycosylated polyamines
Summary: Compounds (I) are useful for treating or preventing cancer such as leukemia, non-small-cell lung cancer, small-cell lung cancer, colon cancer, a cancer of the central nervous system, melanoma, ovarian cancer, breast cancer, renal cancer and prostate cancer.
Novelty: Novel glycosylated polyamines, useful for treating cancer

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