Zobrazeno 1 - 10
of 42
pro vyhledávání: '"Frank P. DiNinno"'
Autor:
Susan P. Rohrer, Edward C. Hayes, Paula M.D. Fitzgerald, Yi Tien Yang, Carolyn DaSilva, Lee-Yuh Pai, Elizabeth T. Birzin, Frank P. DiNinno, Milton L. Hammond, Ralph T. Mosley, Wanda Chan, Liangqin Guo, James M. Schaeffer, Kevin D. Dykstra, Bryan Kraker
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2322-2328
A novel class of indole ligands for estrogen receptor alpha have been discovered which exhibit potent affinity and high selectivity. Substitution of the bazedoxifene skeleton to the linker present in the HTS lead 1a provided 22b which was found to be
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3411966dd884926fb6a499c0d8d428d5
https://doi.org/10.1016/j.bmcl.2007.01.054
https://doi.org/10.1016/j.bmcl.2007.01.054
Autor:
Lee-Yuh Pai, Carolyn DaSilva, Yi Tien Yang, Elizabeth T. Birzin, Ralph T. Mosley, Timothy A. Blizzard, Jerry D. Morgan, Frank P. DiNinno, Edward C. Hayes, Susan P. Rohrer, Milton L. Hammond, Wanda Chan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:5124-5128
Two novel side chains which had previously been found to enhance antagonist activity in the dihydrobenzoxathiin SERM series were applied to three existing platforms. The novel side chains did not improve the antagonist activity of the existing platfo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f6d017a6b688cc1d08c403374f7cf86
https://doi.org/10.1016/j.bmcl.2005.08.084
https://doi.org/10.1016/j.bmcl.2005.08.084
Autor:
Donald B. Kimmel, Lee Yuh Pai, Carolyn DaSilva, Paula M.D. Fitzgerald, Nandini Sharma, Alfred A. Reszka, Wanda Chan, Milton L. Hammond, Elizabeth T. Birzin, Yi Tien Yang, Lawrence F. Colwell, Susan Li, Hilary A. Wilkinson, Sharon Adamski, Qiang Tan, Jerry D. Morgan, Leonard P. Freedman, Edward C. Hayes, James M. Schaeffer, John E. Fisher, Susan P. Rohrer, Timothy A. Blizzard, Frank P. DiNinno, Sudha Warrier, Joel B. Yudkovitz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:1675-1681
The discovery, synthesis, and SAR of chromanes as ERα subtype selective ligands are described. X-ray studies revealed that the origin of the ERα-selectivity resulted from a C-4 trans methyl substitution to the cis-2,3-diphenyl-chromane platform. Se
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ae0224c0d631c57c9693d89abf0b9455
https://doi.org/10.1016/j.bmcl.2005.01.046
https://doi.org/10.1016/j.bmcl.2005.01.046
Autor:
Wanda Chan, Elizabeth T. Birzin, Lee-Yuh Pai, James M. Schaeffer, Edward C. Hayes, Carolyn DaSilva, Susan P. Rohrer, Yi Tien Yang, Frank P. DiNinno, Milton L. Hammond, Jian Liu, Ralph T. Mosley
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:715-718
The ring oxygen and sulfur analogs of lasofoxifene, 1a and 1b, were synthesized in an attempt to impart ERα selectivity, as found in the closely related dihydrobenzoxathiin compound I, recently discovered in these laboratories. The resulting isochro
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::031b4ead375f9a6f4f2ad3a1e8869da3
https://doi.org/10.1016/j.bmcl.2004.11.018
https://doi.org/10.1016/j.bmcl.2004.11.018
Autor:
Milton L. Hammond, Jane Y. Wu, Frank P. DiNinno, Brian Dean, Seongkon Kim, Wei Tang, George A. Doss, Zhoupeng Zhang
Publikováno v:
Organic Letters. 7:411-414
[reaction: see text] During the course of drug metabolism studies, a major metabolite of compound 1 was detected in rhesus monkeys and assigned structure 4. The intriguing biotransformation of 1 leading to 4 was confirmed by a 19-step total synthesis
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0d90d109e68e9ab3dbb2cd4ce6ffc924
https://doi.org/10.1021/ol047741f
https://doi.org/10.1021/ol047741f
Autor:
Frank P. DiNinno, Milton L. Hammond, James M. Schaeffer, Paula M.D. Fitzgerald, Zhoupeng Zhang, Edward C. Hayes, Wanda Chan, Timothy A. Blizzard, Elizabeth T. Birzin, Nandini Sharma, Carolyn DaSilva, Ying Li, Seongkon Kim, Wei Tang, Yi Tien Yang, Jane Y. Wu, Helen Chen, Susan P. Rohrer, Jerry D. Morgan, Lee-Yuh Pai
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:107-113
A series of dihydrobenzoxathiin SERAMs with alkylated pyrrolidine side chains or alkylated linkers was prepared. Minor modifications in the side chain or linker resulted in significant effects on biological activity, especially in uterine tissue.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a7a11661afbd306aacb4d73accdae1e4
https://doi.org/10.1016/j.bmcl.2004.10.036
https://doi.org/10.1016/j.bmcl.2004.10.036
Autor:
Young-Whan Park, Aimie M. Ogawa, Qiang Tan, Katherine Young, Frank P. DiNinno, Ronald E. Painter
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2622-2624
4,7-Dichloro-1-benzothien-2-yl sulfonylaminomethyl boronic acid (DSABA, Compound I ) was discovered as the first boronic acid-based class D beta-lactamase inhibitor. It exhibited an IC 50 of 5.6 μM against OXA-40. The compound also inhibited class A
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4771b047d54ea911dd9958418ca5dead
https://doi.org/10.1016/j.bmcl.2010.02.065
https://doi.org/10.1016/j.bmcl.2010.02.065
Autor:
Frank P. DiNinno, Gregory P. Rouen, Jon G. Sundelof, Joanne B. Laub, Mark L. Greenlee, Joann Huber, Gail G. Hammond, Milton L. Hammond
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:3225-3230
The synthesis and biological evaluation of a series of dicationic-substituted 2-fluorenonylcarbapenems is described. This class of compounds showed enhanced water solubility while maintaining potent activity against MRS. Introduction of a 1-β-methyl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::32811c5ac5a3f04df24eaa1c565a4afa
https://doi.org/10.1016/s0960-894x(99)00567-3
https://doi.org/10.1016/s0960-894x(99)00567-3
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:2973-2976
A series of amidinium-substituted 2-dibenzofuranylcarbapenems with potent activity against MRSA has been synthesized via a Stille cross-coupling reaction. These new carbapenems show reduced serum protein binding and improved in vivo efficacy as a con
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0b0cba274765990296a6392c59ca6997
https://doi.org/10.1016/s0960-894x(99)00526-0
https://doi.org/10.1016/s0960-894x(99)00526-0
Publikováno v:
Tetrahedron Letters. 40:2909-2912
The boron trifluoride-etherate mediated cyclization of 2-arylthio-ketones 1a-h at ambient temperature gave 3-aryl-substituted benzothiophenes 2a-h in excellent yield. None of the rearranged 2-aryl-substituted benzothiophenes were observed.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::76fe9d08a57c9f4a16bdce7b7533dacc
https://doi.org/10.1016/s0040-4039(99)00392-5
https://doi.org/10.1016/s0040-4039(99)00392-5