The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
May. 23, 2017

Filed:

Feb. 03, 2014
Applicant:

University of South Florida, Tampa, FL (US);

Inventors:

Said M. Sebti, Tampa, FL (US);

Srikumar Chellappan, Tampa, FL (US);

Nicholas James Lawrence, Tampa, FL (US);

Assignee:

University of South Florida, Tampa, FL (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07C 279/06 (2006.01); C07C 335/32 (2006.01); C07C 323/45 (2006.01); C07D 233/30 (2006.01); C07D 233/84 (2006.01); C07D 235/08 (2006.01); C07D 249/14 (2006.01); C07D 249/12 (2006.01); C07D 277/42 (2006.01); C07D 277/40 (2006.01); C07D 317/56 (2006.01); C07D 215/12 (2006.01); C07D 213/53 (2006.01); C07D 235/28 (2006.01); C07D 317/58 (2006.01);
U.S. Cl.
CPC ...
C07C 323/45 (2013.01); C07C 279/06 (2013.01); C07C 335/32 (2013.01); C07D 213/53 (2013.01); C07D 215/12 (2013.01); C07D 233/30 (2013.01); C07D 233/84 (2013.01); C07D 235/28 (2013.01); C07D 249/12 (2013.01); C07D 249/14 (2013.01); C07D 277/40 (2013.01); C07D 277/42 (2013.01); C07D 317/56 (2013.01); C07D 317/58 (2013.01);
Abstract

The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with ICvalues ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.


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