Zobrazeno 1 - 10
of 54
pro vyhledávání: '"Arup K. Ghose"'
Publikováno v:
ACS Chemical Neuroscience. 8:147-154
At the discovery stage, it is important to understand the drug design concepts for a CNS drug compared to those for a non-CNS drug. Previously, we published on ideal CNS drug property space and defined in detail the physicochemical property distribut
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::204e25a22d91fc856c902599991a267d
https://doi.org/10.1021/acschemneuro.6b00273
https://doi.org/10.1021/acschemneuro.6b00273
Autor:
Nathan Anderson, Diane E. Gingrich, Arup K. Ghose, Mark S. Albom, Bruce D. Dorsey, Lisa D. Aimone, Elizabeth Bruckheimer, Jason C. Wagner, Matthew A. Curry, Lihui Lu, Jay Friedman, Mark A. Ator, Bruce Ruggeri, Eugen F. Mesaros, Mangeng Cheng, Zeqi Huang, Keith S. Learn, Matthew R. Quail, Thelma S. Angeles, Pawel Dobrzanski, Gregory R. Ott, Sandra V. Fernandez, Joseph G. Lisko, Kevin J. Wells-Knecht, Weihua Wan
Publikováno v:
Journal of medicinal chemistry. 59(16)
Analogues structurally related to anaplastic lymphoma kinase (ALK) inhibitor 1 were optimized for metabolic stability. The results from this endeavor not only led to improved metabolic stability, pharmacokinetic parameters, and in vitro activity agai
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f38d2d8693c2496a71a1241c7558ff6
https://pubmed.ncbi.nlm.nih.gov/27527804
https://pubmed.ncbi.nlm.nih.gov/27527804
Autor:
Henry J. Breslin, Bruce D. Dorsey, Arup K. Ghose, Mangeng Cheng, Mark S. Albom, Kevin J. Wells-Knecht, Weihua Wan, Thelma S. Angeles, R. Curtis Haltiwanger, Brandon M. Lane, Gregory R. Ott
Publikováno v:
Journal of Medicinal Chemistry. 55:449-464
A novel set of 2,4,8,22-tetraazatetracyclo[14.3.1.1(3,7).1(9,13)]docosa-1(20),3(22),4,6,9(21),10,12,16,18-nonaene macrocycles were prepared as potential anaplastic lymphoma kinase (ALK) inhibitors, designed to rigidly lock an energy-minimized bioacti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4dd41a7bcedd19c22f3624560d147f49
https://doi.org/10.1021/jm201333e
https://doi.org/10.1021/jm201333e
Publikováno v:
ACS Chemical Neuroscience
The central nervous system (CNS) is the major area that is affected by aging. Alzheimer's disease (AD), Parkinson's disease (PD), brain cancer, and stroke are the CNS diseases that will cost trillions of dollars for their treatment. Achievement of ap
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9082302be26311a31e107b9e1fc8d1ef
https://doi.org/10.1021/cn200100h
https://doi.org/10.1021/cn200100h
Autor:
Mark S. Albom, Bruce D. Dorsey, Joseph G. Lisko, Mangeng Cheng, Bruce Ruggeri, Arup K. Ghose, Eugen F. Mesaros, Weihua Wan, Mark A. Ator, Matthew R. Quail, Zeqi Huang, Diane E. Gingrich, Tho V. Thieu, Gregory J. Wells, Thelma S. Angeles, Gregory R. Ott, Lisa D. Aimone, Lihui Lu
Publikováno v:
Journal of Medicinal Chemistry. 54:6328-6341
A novel 2,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazine scaffold has been designed as a new kinase inhibitor platform mimicking the bioactive conformation of the well-known diaminopyrimidine motif. The design, synthesis, and validation of this new py
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4ff1dc2c02c706eed915e53603283891
https://doi.org/10.1021/jm200758k
https://doi.org/10.1021/jm200758k
Autor:
Linda Weinberg, Ted L. Underiner, Mark S. Albom, Craig A. Zificsak, Arup K. Ghose, Renee C. Roemmele, Mangeng Cheng, Karen L. Milkiewicz, Jay P. Theroff, Bruce D. Dorsey, Thelma S. Angeles
Publikováno v:
Bioorganic & Medicinal Chemistry. 18:4351-4362
Dysregulation of the anaplastic lymphoma kinase (ALK) is implicated in a variety of cancers. A series of tetrahydropyrido[2,3-b]pyrazines was constructed as ring-constrained analogs of a known aminopyridine kinase scaffold. Chemistry was developed to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b1bddc45e141f6cd00dccf8a2e98b12a
https://doi.org/10.1016/j.bmc.2010.04.087
https://doi.org/10.1016/j.bmc.2010.04.087
Publikováno v:
Journal of Medicinal Chemistry. 51:5149-5171
toward kinase inhibitor discovery, with the result that several kinase inhibitors have been approved as drugs since 2001. The commercial success of imatinib (N-(4-methyl-3-(4-(pyridin-3yl)pyrimidin-2-ylamino)phenyl)-4-((4-methylpiperazin-1-l)methyl)b
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3cfdacb02a80ba9f72c931b97abe0190
https://doi.org/10.1021/jm800475y
https://doi.org/10.1021/jm800475y
Publikováno v:
Drug Discovery Today. 11:1107-1114
The modern drug discovery process is steadily becoming more information driven. Structural, physicochemical and ADME-Tox property profiles of reference (successful) ligands, along with structural information of their target proteins, have been extrem
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8df02ee864149156a10a6701abfd655a
https://doi.org/10.1016/j.drudis.2006.10.012
https://doi.org/10.1016/j.drudis.2006.10.012
Publikováno v:
Journal of Receptors and Signal Transduction. 21:357-375
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5ba17614e626928c6e12c4c198b4569e
https://doi.org/10.1081/rrs-100107923
https://doi.org/10.1081/rrs-100107923
Publikováno v:
Perspectives in Drug Discovery and Design. 19:85-98
Methods for the calculation of two properties of interest in drug design, namely free energy of aqueous solvation and lipophilicity (log P), using fragmental methods are reviewed here. Though aqueous solvation free energies are commonly estimated usi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6ba5c9c9af121c886bf2e300bd0b0bfa
https://doi.org/10.1023/a:1008767505932
https://doi.org/10.1023/a:1008767505932