dc.contributor.author | Kambhampati, Suman | |
dc.contributor.author | Rajewski, Roger A. | |
dc.contributor.author | Tanol, Mehmet | |
dc.contributor.author | Haque, Inamul | |
dc.contributor.author | Das, Amlan | |
dc.contributor.author | Bangerjee, Snigdha | |
dc.contributor.author | Jha, Saheli | |
dc.contributor.author | Burns, Douglas | |
dc.contributor.author | Reyes, Emma Borrego-Diaz | |
dc.contributor.author | Van Veldhuizen, Peter J. | |
dc.contributor.author | Banerjee, Sushanta K. | |
dc.date.accessioned | 2016-02-12T21:55:17Z | |
dc.date.available | 2016-02-12T21:55:17Z | |
dc.date.issued | 2016-01-27 | |
dc.identifier.citation | Kambhampati, S., R. A. Rajewski, M. Tanol, I. Haque, A. Das, S. Banerjee, S. Jha, D. Burns, E. Borrego-Diaz, P. J. Van Veldhuizen, and S. K. Banerjee. "A Second-Generation 2-Methoxyestradiol Prodrug Is Effective against Barrett's Adenocarcinoma in a Mouse Xenograft Model." Molecular Cancer Therapeutics 12.3 (2013): 255-63. http://dx.doi.org/10.1158/1535-7163.MCT-12-0777 | en_US |
dc.identifier.uri | http://hdl.handle.net/1808/20074 | |
dc.description | This is the author's accepted manuscript. The original is available at http://mct.aacrjournals.org/content/12/3/255 | en_US |
dc.description.abstract | 2-Methoxyestradiol (2-ME2) is an endogenous metabolite of estradiol. In preclinical models, 2-ME2 is effective against different types of tumors. Unfortunately, only low systemic concentrations of 2-ME2 can be achieved following oral administration, even after very high doses are administered to patients. In an effort to solve this problem we have now synthesized and tested a new prodrug of 2-ME2 that is water soluble due to a bio-reversible hydrophilic group added at the 3-position and more effectively resists metabolic inactivation due to an ester moiety added to mask the 17-position alcohol. We are reporting here for the first time that this double prodrug of 2-ME2 is effective as an antiproliferative and anti-cancer agent for both in vitro and in vivo studies against Barrett's esophageal adenocarcinoma (BEAC), and provided greater potency than 2-ME2 in inhibiting the growth of BEAC xenografts. Finally, studies indicate that, like 2-ME2, the 2-ME2-PD1 exhibits anticancer effect through possible disruption of microtubule-network. | en_US |
dc.publisher | American Association for Cancer Research | en_US |
dc.subject | 2-Methoxyestradiol | en_US |
dc.subject | Esophageal cancer | en_US |
dc.subject | Chemotherapy | en_US |
dc.subject | Prodrug | en_US |
dc.title | A Second Generation 2-Methoxyestradiol Prodrug Is Effective Against Barrett's Adenocarcinoma in a Mouse Xenograft Model | en_US |
dc.type | Article | |
kusw.kuauthor | Rajewski, Roger A. | |
kusw.kudepartment | Pharmaceutical Chemistry | en_US |
dc.identifier.doi | 10.1158/1535-7163.MCT-12-0777 | |
kusw.oaversion | Scholarly/refereed, author accepted manuscript | |
kusw.oapolicy | This item meets KU Open Access policy criteria. | |
dc.rights.accessrights | openAccess | |