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Autor:
Robert N. Hanson, Nisal Gajadeera
Publikováno v:
Steroids. 145:39-46
A set of derivatives of 11β-(4-oxyphenyl)estradiol were prepared as potential fluorescent imaging agents for the evaluation of the estrogen receptor. The compounds were designed based on the established affinity and selectivity of 11β-[4-(dimethyle
Autor:
Nisal Gajadeera, Robert N. Hanson
Publikováno v:
Steroids. 144:30-46
The development of fluorescent ligands for the estrogen receptor (ER) continues to be of interest. Over the past 20 years, most efforts have focused on appending an expanding variety of fluorophores to the B-, C- and D-rings of the steroidal scaffold
Autor:
Timothy A. Coulther, David Labaree, Jessa L. Silver, Robert Dilis, Edward Hua, Richard B. Hochberg, Emmett McCaskill, Robert N. Hanson, Mary Jo Ondrechen, Pakamas Tongcharoensirikul
Publikováno v:
Steroids. 144:15-20
A series consisting of substituted benzoylbenzamide derivatives of 17α-E-vinyl estradiol 6a-i and 7a-d was prepared in good overall yields from the corresponding novel iodinated benzoylbenzamide precursors using Pd(0)-catalyzed Stille coupling. Biol
Autor:
Kelton Barnsley, Robert N. Hanson, Mary Jo Ondrechen, Eugene R. DeSombre, Alun Hughes, Pakamas Tongcharoensirikul
Publikováno v:
Steroids. 96:50-62
A series of three 1,1-bis(4-hydroxyphenyl)-2-(3-hydroxyphenyl)-ethylene derivatives was prepared and evaluated as potential estrogen receptor imaging agents. The compounds display high binding affinity compared to estradiol, with the 2-iodo and 2-bro
Publikováno v:
Bioorganic & Medicinal Chemistry. 22:917-926
A series of unsymmetrically substituted biphenyl compounds was designed as alpha helical proteomimetics with the aim of inhibiting the binding of coactivator proteins to the nuclear hormone receptor coactivator binding domain. These compounds were sy
Autor:
Emily B. Corcoran, Robert N. Hanson
Publikováno v:
Medicinal Research Reviews. 34:596-643
In an effort to discover a noninvasive method for predicting which cancer patients will benefit from therapy targeting the EGFR and HER2 proteins, a large body of the research has been conducted toward the development of PET and SPECT imaging agents,
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:6587-6590
A series of bipolar biphenyl compounds was synthesized as proteomimetic analogs of the LXXLL penta-peptide motif responsible for the binding of coactivator proteins to the nuclear hormone receptor coactivator binding domain. These compounds were subj
Autor:
Anna B. Williams, Robert N. Hanson
Publikováno v:
Tetrahedron. 68:5406-5414
As part of our ongoing project to develop new molecular probes for estrogen receptor-alpha, we are exploring the utility of internally-substituted asymmetric biphenyls as a proteomimetic scaffold. In this study, we describe synthetic methods for prep