Zobrazeno 1 - 10
of 30
pro vyhledávání: '"Ron Bihovsky"'
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1151-1155
A series of novel pyrrolocarbazole lactams was identified as potent PARP-1 inhibitors in vitro and in a PC12 cellular NAD(+) depletion assay. The SAR trends of substituents at the 3-position, as well as the effect of blocking the indole or lactam NH-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bc5a498bb7b7d8aa98fd6614bcc5aa77
https://doi.org/10.1016/j.bmcl.2005.11.086
https://doi.org/10.1016/j.bmcl.2005.11.086
Autor:
Mark A. Ator, Gregory J. Wells, Ming Tao, Robert L. Hudkins, Jean Husten, Chung Ho Park, Ron Bihovsky
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:938-942
A series of novel pyrrolocarbazoles was synthesized as potential PARP-1 inhibitors. Pyrrolocarbazole 1 was identified as a potent PARP-1 inhibitor (IC50 = 36 nM) from our internal database. Synthesis of analogs around this template with the aid of mo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c35140b2fb10455bb87f2371800e7068
https://doi.org/10.1016/j.bmcl.2005.10.099
https://doi.org/10.1016/j.bmcl.2005.10.099
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:1035-1038
A series of potent 1,2-benzothiazine 1,1-dioxide alpha-ketoamide inhibitors of calpain I is described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::baad317b72d0a2921235b31e3a678fac
https://doi.org/10.1016/j.bmcl.2003.11.037
https://doi.org/10.1016/j.bmcl.2003.11.037
Publikováno v:
Journal of Medicinal Chemistry. 44:3488-3503
A series of peptide mimetic aldehyde inhibitors of calpain I was prepared in which the P(2) and P(3) amino acids were replaced by substituted 3,4-dihydro-1,2-benzothiazine-3-carboxylate 1,1-dioxides. The effect of 2, 6, and 7-benzothiazine substituen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::790737c6aa36abf2d15d8f52145b1328
https://doi.org/10.1021/jm010178b
https://doi.org/10.1021/jm010178b
Autor:
Robert Siman, Derek Dunn, Ming Tao, Sankar Chatterjee, Zi-Qiang Gu, Gregory J. Wells, Mark A. Ator, John P. Mallamo, Ron Bihovsky
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:2371-2374
A series of potent P2-achiral, P'-extended alpha-ketoamide inhibitors of calpain I is described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99cf123a6891f9684c63e2a9eb7790f8
https://doi.org/10.1016/s0960-894x(99)00392-3
https://doi.org/10.1016/s0960-894x(99)00392-3
Autor:
Gregory J. Wells, Ron Bihovsky
Publikováno v:
Expert Opinion on Therapeutic Patents. 8:1707-1727
Calpain, a calcium-activated cysteine protease present in most mammalian tissues, including the brain, has been implicated in neurodegenerative processes resulting from its overactivation following cerebral ischaemia or traumatic injury to the head o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9d540e538774a135967de1b2df5bb4da
https://doi.org/10.1517/13543776.8.12.1707
https://doi.org/10.1517/13543776.8.12.1707
Publikováno v:
Journal of Medicinal Chemistry. 41:3912-3916
Dipeptidyl phosphorus compounds were synthesized as potential bioisosteric mimics of peptide alpha-ketoesters and alpha-ketoacids. alpha-Ketophosphonate Cbz-Leu-Leu-P(O)(OCH3)2 (1b), containing an alpha-ketoester bioisostere, inhibits human calpain I
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::10d9042795270fab09c2a0a14b256a37
https://doi.org/10.1021/jm980325e
https://doi.org/10.1021/jm980325e
Autor:
Kurt A. Josef, Donna Bozyczko-Coyne, Zi-Qiang Gu, Sankar Chatterjee, Ming Tao, Rabindranath Tripathy, Ron Bihovsky, Mark A. Ator, Beth Ann McKenna, Shobha E. Senadhi, John P. Mallamo, Teresa M. O'Kane, Satish Mallya, Robert Siman, Derek Dunn
Publikováno v:
Journal of Medicinal Chemistry. 41:2663-2666
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::602925a84b28f1f6315385e1e320e622
https://doi.org/10.1021/jm980035y
https://doi.org/10.1021/jm980035y
Autor:
Shobha E. Senadhi, Eric Griffith, Sheryl L. Meyer, Rabindranath Tripathy, William Biazzo, Sankar Chatterjee, Kurt A. Josef, Manoj Das, Bruce Dembofsky, Bethany Freed, Ming Tao, Patricia A. Messina, Robert Siman, Derek Dunn, Mark A. Ator, Ron Bihovsky, Mohamed Iqbal, Donna Bozyczko-Coyne
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:539-544
Dipeptide and tripeptide aldehydes have been evaluated as inhibitors of human calpain I. Dipeptide aldehydes are generally equipotent with tripeptide aldehydes. Calpain I possesses a rather stringent requirement for Leu at P2, but accepts a variety o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::969c79285bb942274ed65d64259fb405
https://doi.org/10.1016/s0960-894x(97)00063-2
https://doi.org/10.1016/s0960-894x(97)00063-2
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:3009-3012
Dipeptidyl and tripeptidyl heterocycles designed to mimic peptide ketoanides and ketoacids were prepared and evaluated in vitro as inhibitors of human calpain I. Boc-Leu-Leu-imidazole ( 12 ) inhibited calpain I at low micromolar concentrations.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::bf4a3823be3dcdf4541a1765fb921ba3
https://doi.org/10.1016/s0960-894x(96)00550-1
https://doi.org/10.1016/s0960-894x(96)00550-1