Zobrazeno 1 - 10
of 35
pro vyhledávání: '"Carl Crysler"'
Autor:
Christopher J. Molloy, Bruce E. Tomczuk, Danielle Lawrence, Christian Baumann, Heidi Ott, Shelley K. Ballentine, Jinsheng Chen, Mark J. Wall, Kenneth J. Wilson, Sanath K. Meegalla, Lisa Boczon, Edward J. Yurkow, Yanmin Chen, Carl Crysler, Lee Zeng, Carol F. Franks, Robert R. Donatelli, Margery A. Chaikin, Judith F. Baker, Zhao Zhou, Robert W. Tuman, Carl R. Illig, Dana L. Johnson, Carl L. Manthey
There is increasing evidence that tumor-associated macrophages promote the malignancy of some cancers. Colony-stimulating factor-1 (CSF-1) is expressed by many tumors and is a growth factor for macrophages and mediates osteoclast differentiation. Her
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::da7c495ed76df00defda047352171a57
https://doi.org/10.1158/1535-7163.c.6531858.v1
https://doi.org/10.1158/1535-7163.c.6531858.v1
Autor:
Jeremy M. Travins, Carl Crysler, Hufnagel Heather Rae, Karen DiLoreto, Norman Huebert, Michael X. Kolpak, Nalin L. Subasinghe, Jennifer Kirkpatrick, Stephen H. Eisennagel, Bruce E. Tomczuk, Wenxi Pan, Christopher J. Molloy, Ehab Khalil, Nisha S. Ninan, Shelley K. Ballentine, Kristi A. Leonard, Roger F. Bone, Richard Soll, Farah Ali, Michael D. Gaul
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:5303-5307
Complement C1s protease inhibitors have potential utility in the treatment of diseases associated with activation of the classical complement pathway such as humorally mediated graft rejection, ischemia-reperfusion injury (IRI), vascular leak syndrom
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::44891a19d07c75d5617cf44b0ba3e337
https://doi.org/10.1016/j.bmcl.2012.06.030
https://doi.org/10.1016/j.bmcl.2012.06.030
Autor:
Cuifen Hou, Evan Opas, Dana L. Johnson, Monica Singer, Carl Crysler, James C. Lanter, Zhihua Sui, Fu-An Kang, Sandra McKenney, Xuqing Zhang, Nalin L. Subasinghe, Thomas P. Markotan, Christopher J. Molloy
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:7496-7501
As a result of further SAR studies on a piperidinyl piperidine scaffold, we report the discovery of compound 44, a potent, orally bioavailable CCR2 antagonist. While having some in vitro hERG activity, this molecule was clean in an in vivo model of Q
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c5df78b7755aa9a1b0fc035055841ee6
https://doi.org/10.1016/j.bmcl.2011.09.113
https://doi.org/10.1016/j.bmcl.2011.09.113
Autor:
Christopher J. Molloy, Shelley K. Ballentine, Edward J. Yurkow, Carsten Schubert, Carl Crysler, Renee L. DesJarlais, Yanmin Chen, Sanath K. Meegalla, Carl L. Manthey, Mark J. Wall, Bruce E. Tomczuk, Carl R. Illig, Zhao Zhou, Jinsheng Chen, Kenneth J. Wilson, Mark R. Player, Robert R. Donatelli, Margery A. Chaikin
Publikováno v:
Journal of Medicinal Chemistry. 54:7860-7883
A class of potent inhibitors of colony-stimulating factor-1 receptor (CSF-1R or FMS), as exemplified by 8 and 21, was optimized to improve pharmacokinetic and pharmacodynamic properties and potential toxicological liabilities. Early stage absorption,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::dea3adaebd4f6f20559806e92e11896f
https://doi.org/10.1021/jm200900q
https://doi.org/10.1021/jm200900q
Autor:
Zhihua Sui, Xuqing Zhang, Evan Opas, Hufnagel Heather Rae, Dana L. Johnson, Carl Crysler, Cuifen Hou, Sandra McKenney, John O’Neill
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6042-6048
A novel series of 4-azetidinyl-1-aryl-cyclohexanes containing indazole or benzoisoxazole moiety have been identified as potent CCR2 antagonists with high selectivity versus hERG.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c2d5bf1e30a29a9e435c550c9359fa0c
https://doi.org/10.1016/j.bmcl.2011.08.074
https://doi.org/10.1016/j.bmcl.2011.08.074
Autor:
Zhihua Sui, Evan Opas, Cuifen Hou, Carl Crysler, Monica Singer, Xuqing Zhang, Dana L. Johnson, Chaozhong Cai, Hufnagel Heather Rae, Thomas P. Markotan, Sandra McKenney, James C. Lanter
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5577-5582
A series of 4-azetidinyl-1-aryl-cyclohexanes as potent CCR2 antagonists with high selectivity over activity for the hERG potassium channel is discovered through divergent SARs of CCR2 and hERG.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::13350ab536cad7aa9c759b2b60a1aa24
https://doi.org/10.1016/j.bmcl.2011.06.080
https://doi.org/10.1016/j.bmcl.2011.06.080
Autor:
Danielle Lawrence, Yanmin Chen, Mark J. Wall, Carl L. Manthey, Christopher J. Molloy, Edward J. Yurkow, Kenneth J. Wilson, Sanath K. Meegalla, Dana L. Johnson, Carol F. Franks, Bruce E. Tomczuk, Lee Zeng, Shelley K. Ballentine, Baumann Christian Andrew, Zhao Zhou, Judith Baker, Robert R. Donatelli, Lisa Boczon, Carl Crysler, Carl R. Illig, Heidi Ott, Jinsheng Chen, Tuman Robert W, Margery A. Chaikin
Publikováno v:
Molecular Cancer Therapeutics. 8:3151-3161
There is increasing evidence that tumor-associated macrophages promote the malignancy of some cancers. Colony-stimulating factor-1 (CSF-1) is expressed by many tumors and is a growth factor for macrophages and mediates osteoclast differentiation. Her
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3a1dcd64b489777dd1393ee065709ba7
https://doi.org/10.1158/1535-7163.mct-09-0255
https://doi.org/10.1158/1535-7163.mct-09-0255
Autor:
Yanmin Chen, Christopher J. Molloy, Carl R. Illig, Margery A. Chaikin, Carl L. Manthey, Renee L. DesJarlais, Carl Crysler, Carsten Schubert, Sanath K. Meegalla, Mark R. Player, Jinsheng Chen, Shelley K. Ballentine, Bruce E. Tomczuk, Mark J. Wall, Kenneth J. Wilson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3632-3637
An anti-inflammatory 1,2,4-phenylenetriamine-containing series of FMS inhibitors with a potential to form reactive metabolites was transformed into a series with equivalent potency by incorporation of carbon-based replacement groups. Structure-based
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ae7fedad7a5539d69102e1d1474ac077
https://doi.org/10.1016/j.bmcl.2008.04.059
https://doi.org/10.1016/j.bmcl.2008.04.059
Autor:
Renee L. DesJarlais, Carl R. Illig, Shelley K. Ballentine, Margery A. Chaikin, M. Jonathan Rudolph, Carsten Schubert, Kenneth J. Wilson, Bruce E. Tomczuk, Jinsheng Chen, Mark R. Player, Ioanna Petrounia, Mark J. Wall, Christopher J. Molloy, Yanmin Chen, Sanath K. Meegalla, Carl Crysler, Carl L. Manthey
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1642-1648
The optimization of the arylamide lead 2 resulted in identification of a highly potent series of 2,4-disubstituted arylamides. Compound 8 (FMS kinase IC(50)=0.0008 microM) served as a proof-of-concept candidate in a collagen-induced model of arthriti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8bc7fcf0d95c0b945a2cac5006d4cedc
https://doi.org/10.1016/j.bmcl.2008.01.059
https://doi.org/10.1016/j.bmcl.2008.01.059
Autor:
Renee L. DesJarlais, Hui Huang, Jennifer Kirkpatrick, Nalin L. Subasinghe, Norman Huebert, Gaul Michael David, Nisha S. Ninan, Joan Gushue, Jeremy M. Travins, Bruce E. Tomczuk, Roger F. Bone, Shelley K. Ballentine, Christopher J. Molloy, Kristi A. Leonard, Ehab Khalil, Hufnagel Heather Rae, Farah Ali, Maxwell D. Cummings, Richard M. Soll, Wenxi Pan, Carl Crysler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1603-1606
Complement activation has been implicated in disease states such as hereditary angioedema, ischemia-reperfusion injury, acute respiratory distress syndrome, and acute transplant rejection. Even though the complement cascade provides several protein t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::06eefcfefc962ecd7776e95a4980fdd8
https://doi.org/10.1016/j.bmcl.2008.01.064
https://doi.org/10.1016/j.bmcl.2008.01.064