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:
Oct. 06, 2020

Filed:

Nov. 18, 2015
Applicant:

University of Maryland, Baltimore, Baltimore, MD (US);

Inventors:

Vincent Njar, Glen Burnie, MD (US);

Hannah Mbatia, Germantown, MD (US);

Vidya Ramamurthy, Baltimore, MD (US);

Senthilmurugan Ramalingam, Baltimore, MD (US);

Assignee:

UNIVERSITY OF MARYLAND, BALTIMORE, Baltimore, MD (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
A61K 31/4164 (2006.01); A61K 31/165 (2006.01); A61K 31/203 (2006.01); A61K 31/215 (2006.01); A61K 31/4406 (2006.01); A61K 31/505 (2006.01); A61K 31/4409 (2006.01); C07D 233/56 (2006.01); C07D 239/26 (2006.01); C07D 213/56 (2006.01); C07C 403/20 (2006.01); A61P 35/00 (2006.01); C07D 213/55 (2006.01);
U.S. Cl.
CPC ...
C07D 233/56 (2013.01); A61K 31/165 (2013.01); A61K 31/203 (2013.01); A61K 31/215 (2013.01); A61K 31/4164 (2013.01); A61K 31/4406 (2013.01); A61K 31/4409 (2013.01); A61K 31/505 (2013.01); A61P 35/00 (2018.01); C07C 403/20 (2013.01); C07D 213/55 (2013.01); C07D 213/56 (2013.01); C07D 239/26 (2013.01); C07C 2601/16 (2017.05);
Abstract

The synthesis and in vitro and in vivo anti-breast and anti-prostate cancers activities of novel C-4 heteroaryl 13-cis retinamides that modulate Mnk-eIF4E and AR signaling are discussed. In both breast and prostate cancer cell lines, these compounds induce Mnk1/2 degradation to substantially suppress eIF4E phosphorylation. In prostate cancer cells, the compounds induce degradation of both full-length androgen receptor (fAR) and splice variant AR (AR-V7) to inhibit AR transcriptional activity. The consequences of these multiple activities resulted in inhibition of cell growth and migration and induction of apoptosis. Finally and importantly, the compounds demonstrate strong in vitro and in vivo anti-breast and anti-prostate cancer activities, with no apparent host toxicities.


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