Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Collin F. Regan"'
Autor:
Fabrice Pierre, Collin F. Regan, David M. Ryckman, Mustapha Haddach, Michael K. Schwaebe, Michael E. Jung
Publikováno v:
Synlett. 23:443-447
This paper reports the synthesis of various 5-halopyrimidine-4-carboxylic acid esters via the Minisci homolytic alkoxycarbonylation of 5-halopyrimidines. The reaction was found to be highly regioselective, allowing the one-step synthesis of useful am
Autor:
Denis Drygin, Jerome Michaux, Fabrice Pierre, Diwata Macalino, Mustapha Haddach, Cosmin Borsan, David M. Ryckman, Collin F. Regan, Sean O'Brien, Pauline Kerdoncuff, Eric Stefan, Adam Siddiqui-Jain, Peter C. Chua, Michael K. Schwaebe, William G. Rice
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:45-48
Protein kinase CK2 is a potential drug target for many diseases including cancer and inflammation disorders. The crystal structure of clinical candidate CX-4945 1 with CK2 revealed an indirect interaction with the protein through hydrogen bonding bet
Autor:
Denis Drygin, Marie-Claire Chevrel, Anne‐Sophie Nedellec, Collin F. Regan, Diwata Macalino, Mustapha Haddach, Sean O'Brien, Adam Siddiqui-Jain, Kenna Anderes, Fabrice Pierre, Eric Stefan, Nicole Streiner, David M. Ryckman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6687-6692
A novel class of pan-Pim kinase inhibitors was designed by modifying the CK2 inhibitor CX-4945. Introduction of a triazole or secondary amide functionality on the C-7 position and 2'-halogenoanilines on C-5 resulted in potent inhibitors of the Pim-1
Autor:
Fabio C. Tucci, Martin W. Rowbottom, Susan K. Sullivan, R. Scott Struthers, Yang Sai, Collin F. Regan, Shelby Reijmers, Chen Chen, Zhiqiang Guo, Qiu Xie, Dongpei Wu, Yun-Fei Zhu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:3685-3690
SAR studies of 1,3,5-triazine-2,4,6-triones as human gonadotropin-releasing hormone receptor antagonists resulted in potent compounds. The best compound from the series had a binding affinity of 2 nM.
Publikováno v:
Angewandte Chemie. 125:2114-2116
ChemInform Abstract: Se-Phenyl Prop-2-eneselenoate: An Ethylene Equivalent for Diels-Alder Reactions
Publikováno v:
ChemInform. 44
others. [7] In an approach to the total synthesis of brasilicardin A, 1, [8] we needed an ethylene equivalent for the preparation of the C ring. Since many of the known ethylene equivalents did not work well for various reasons, we decided to develop
Publikováno v:
Angewandte Chemie (International ed. in English). 52(7)
others. [7] In an approach to the total synthesis of brasilicardin A, 1, [8] we needed an ethylene equivalent for the preparation of the C ring. Since many of the known ethylene equivalents did not work well for various reasons, we decided to develop
Autor:
Collin F. Regan, Mustapha Haddach, Fabrice Pierre, Michael E. Jung, Michael K. Schwaebe, David M. Ryckman
Publikováno v:
ChemInform. 43
A convenient one-pot procedure is developed for the synthesis of the title compounds, where ester (II) is found to be optimal for the process.
Autor:
Collin F. Regan, Sean O'Brien, Denis Drygin, Adam Siddiqui-Jain, David M. Ryckman, Diwata Macalino, William G. Rice, Mustapha Haddach, Nicole Streiner, Marie-Claire Chevrel, Fabrice Pierre
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(9)
A novel family of potent dual inhibitors of CK2 and the Pim kinases was discovered by modifying the scaffolds of tricyclic Pim inhibitors. Several analogs were active at single digit nanomolar IC50 values against CK2 and the Pim isoforms Pim-1 and Pi
Autor:
Tomas Szabo, James R. McCarthy, Dimitri E. Grigoriadis, Collin F. Regan, Brian Dyck, Dragan Marinkovic, Xiaohu Zhang, Michael K. Schwaebe, Mustapha Haddach, Raymond S. Gross, Manisha Moorjani, John Saunders, John P. Williams, Haig Bozigian, Zhiqiang Guo, Ta Kung Chen
Publikováno v:
Journal of medicinal chemistry. 48(12)
Two new classes of tricyclic-based corticotropin-releasing factor (CRF(1)) receptor-1 antagonists were designed by constraining known 1H-pyrrolo[2,3-b]pyridine and 1H-pyrazolo[3,4-b]pyridine ligands. Pyrrole- and pyrazole-based molecules 19g and 22a,