824946-76-1Relevant academic research and scientific papers
Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of 2-methoxyestradiol
Agoston, Gregory E.,Shah, Jamshed H.,Suwandi, Lita,Hanson, Arthur D.,Zhan, Xiaoguo,LaVallee, Theresa M.,Pribluda, Victor,Treston, Anthony M.
, p. 6241 - 6244 (2009)
The syntheses of 21 analogs of 2-methoxyestradiol are presented, including ENMD-1198 which was selected for advancement into Phase 1 clinical trials in oncology. These analogs were evaluated for antiproliferative activity using breast tumor MDA-MB-231 cells, for antiangiogenic activity in HUVEC proliferation assays, and for estrogenic activity in MCF-7 cell proliferation. The most active analogs were evaluated for iv and oral pharmacokinetic properties via cassette dosing in rat and in mice pharmacokinetic models.
Synthesis and antitumor activities of 3-modified 2-methoxyestradiol analogs
Suwandi, Lita S.,Agoston, Gregory E.,Shah, Jamshed H.,Hanson, Arthur D.,Zhan, Xiaoguo H.,LaVallee, Theresa M.,Treston, Anthony M.
scheme or table, p. 6459 - 6462 (2010/05/02)
The syntheses of 2-methoxyestradiol analogs with modifications at the 3-position are described. The analogs were assessed for their antiproliferative, antiangiogenic, and estrogenic activities. Several lead substituents were identified with similar or imp
Antiangiogenic agents
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Page 34, (2010/02/10)
Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering compounds of the general formula: wherein the variables are defined in the specification.
