Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Mike Frohn"'
Autor:
Andrew Tasker, Andrea Itano, Anu Gore, Paul E. Harrington, Mike Frohn, Victor J. Cee, Michele McElvain, Min Wong, Mike Fiorino, Alexander J. Pickrell, Kelvin K. C. Sham, Han Xu, Brian A. Lanman, Anthony B. Reed, Yang Xu, Susana C. Neira, Scot Middleton, Henry Morrison
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1779-1783
Replacement of the azetidine carboxylate of an S1P1 agonist development candidate, AMG 369, with a range of acyclic head-groups led to the identification of a novel, S1P3-sparing S1P1 agonist, (−)-2-amino-4-(3-fluoro-4-(5-(1-phenylcyclopropyl)thiaz
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::00f3cc5bea5e6a249ac305b5230ca5f2
https://doi.org/10.1016/j.bmcl.2011.12.073
https://doi.org/10.1016/j.bmcl.2011.12.073
Autor:
Michael Croghan, Andrew Tasker, Matthew R. Lee, Xuxia Zhang, Heather A. Arnett, Victor J. Cee, Anthony B. Reed, Kelvin K. C. Sham, Michele McElvain, Henry Morrison, Alexander J. Pickrell, Lewis D. Pennington, Mike Frohn, Yang Xu, Paul E. Harrington, Min Wong, Han Xu, Brian A. Lanman, Mike Fiorino, Christopher H. Fotsch
Publikováno v:
ACS Medicinal Chemistry Letters. 3:74-78
The optimization of a series of S1P1 agonists with limited activity against S1P3 is reported. A polar headgroup was used to improve the physicochemical and pharmacokinetic parameters of lead quinolinone 6. When dosed orally at 1 and 3 mg/kg, the azah
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::513454b43d7abc3801057fdc295f1e0a
https://doi.org/10.1021/ml200252b
https://doi.org/10.1021/ml200252b
Autor:
Min Wong, Yang Xu, Scot Middleton, Matthew R. Lee, Anu Gore, Mike Fiorino, Alex Pickrell, Kristine M. Muller, Andrea Itano, Mike Frohn, Heather A. Arnett, Janet Buys, Michelle Horner, Dalia Rivenzon-Segal, Jennifer E. Golden, Victor J. Cee, Hugo M. Vargas, Roland Burli, Susana C. Neira, Michael Schrag, Han Xu, Brian A. Lanman, Michele McElvain, Xuxia Zhang, Jerry Siu
Publikováno v:
ACS Medicinal Chemistry Letters. 2:107-112
The optimization of a series of thiazolopyridine S1P1 agonists with limited activity at the S1P3 receptor is reported. These efforts resulted in the discovery of 1-(3-fluoro-4-(5-(1-phenylcyclopropyl)thiazolo-[5,4-b]pyridin-2-yl)benzyl)azetidine-3-ca
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::469aac7dbf0531b12b4eec83f252b55d
https://doi.org/10.1021/ml100306h
https://doi.org/10.1021/ml100306h
Autor:
Jennifer E. Golden, Randall W. Hungate, Alexander J. Pickrell, Gloria Biddlecome, Roland Burli, Mike Frohn, Jennifer Dao, Norma Rogers, Vellarkad N. Viswanadhan, Jennifer R. Allen, Kristine M. Muller, Sean Yoder
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5023-5026
We report the structure-based design and synthesis of a novel series of aza-benzimidazoles as PHD2 inhibitors. These efforts resulted in compound 22, which displayed highly potent inhibition of PHD2 function in vitro.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6fe8ee6a4b24c934b0f90897c408cc8
https://doi.org/10.1016/j.bmcl.2008.08.012
https://doi.org/10.1016/j.bmcl.2008.08.012
Autor:
Kelly Regal, Randall W. Hungate, Mike Frohn, Vellarkad N. Viswanadhan, Matthew Adlam, Han Xu, Philip Tagari, Min Wong, Kristine M. Muller, Roland Burli, Jennifer E. Golden, Xiaoming Zou, Matthew H. Plant, Michele McElvain
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:3713-3718
We report the discovery of potent agonists for the human formyl-peptide-like 1 receptor (hFPRL1). These compounds did not act at a closely related receptor denoted human formyl peptide receptor (hFPR) up to 10 microM concentration. Recent studies hav
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d19e4048cb68caaf96dd2c0a6c5b8b6a
https://doi.org/10.1016/j.bmcl.2006.04.068
https://doi.org/10.1016/j.bmcl.2006.04.068
Publikováno v:
The AAPS journal. 17(1)
Glycation of therapeutic proteins occurs during mammalian cell culture expression and upon administration to patients. Since the chemical attachment of mannose or other sugars via a chemical linker has been shown to increase a protein’s clearance r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d6de333d6a3572df06d063ad8b48912d
https://pubmed.ncbi.nlm.nih.gov/25413724
https://pubmed.ncbi.nlm.nih.gov/25413724
Publikováno v:
Tetrahedron Letters. 48:487-489
An efficient synthetic route to 1,6- and 1,7-dibromo-3-aminoisoquinoline was devised. These intermediates served as ideal templates for the preparation of 3-aminoisoquinoline analogues functionalized at C(6) or C(7).
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6428f8b0410b31771c9b58694ab1b3f5
https://doi.org/10.1016/j.tetlet.2006.11.035
https://doi.org/10.1016/j.tetlet.2006.11.035
Autor:
John G. Allen, Andreas Reichelt, Guomin Yao, Julie M. Bailis, Elizabeth M. Doherty, James R. Falsey, Tisha San Miguel, Leeanne Zalameda, Marian C. Bryan, Michael D. Bartberger, Mike Frohn
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(7)
Cdc7 kinase is responsible for the initiation and regulation of DNA replication and has been proposed as a target for cancer therapy. We have identified a class of Cdc7 inhibitors based on a substituted indole core. Synthesis of focused indole and az
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2a0bec87ac4e6199252766c6b352f4c1
https://pubmed.ncbi.nlm.nih.gov/23481650
https://pubmed.ncbi.nlm.nih.gov/23481650
Autor:
Mike, Frohn, Victor J, Cee, Brian A, Lanman, Alexander J, Pickrell, Jennifer, Golden, Dalia, Rivenzon-Segal, Scot, Middleton, Mike, Fiorino, Han, Xu, Michael, Schrag, Yang, Xu, Michele, McElvain, Kristine, Muller, Jerry, Siu, Roland, Bürli
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(1)
An SAR campaign designed to increase polarity in the 'tail' region of benzothiazole 1 resulted in two series of structurally novel 5-and 6-substituted S1P(1) agonists. Structural optimization for potency ultimately delivered carboxamide (+)-11f, whic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::a247b4fe72d40dd1e5f354990a4182dd
https://pubmed.ncbi.nlm.nih.gov/22100314
https://pubmed.ncbi.nlm.nih.gov/22100314
Autor:
Michelle Horner, Kristine M. Muller, Xuxia Zhang, Xiang Yu, Nili Schutz, Jerry Siu, Dalia Rivenzon-Segal, Roland Burli, Zhang Zhaoda, Susana C. Neira, Hugo M. Vargas, Alexander J. Pickrell, Jennifer E. Golden, Yang Xu, Victor J. Cee, Michael Schrag, Scot Middleton, Jian Lin, Yael Marantz, Andrea Itano, Mercedes Lobera, Han Xu, Brian A. Lanman, Michele McElvain, Janet Buys, Anu Gore, Srinivasa R Cheruku, Anurag Sharadendu, Mike Fiorino, Mike Frohn
Optimization of a benzofuranyl S1P1 agonist lead compound (3) led to the discovery of 1-(3-fluoro-4-(5-(2-fluorobenzyl)benzo[d]thiazol-2-yl)benzyl)azetidine-3-carboxylic acid (14), a potent S1P1 agonist with minimal activity at S1P3. Dosed orally at
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4114b66ba763963fd644e7ff1f508317
https://europepmc.org/articles/PMC4018108/
https://europepmc.org/articles/PMC4018108/
