Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Nirmala Raghavan"'
Autor:
Matthew D. Hill, Haiquan Fang, Derek Norris, George V. Delucca, Hong Huang, Mikkel DeBenedetto, Claude Quesnelle, William D. Schmitz, John S. Tokarski, Steven Sheriff, Chunhong Yan, Caroline Fanslau, Zuzana Haarhoff, Christine Huang, Melissa Kramer, Shilpa Madari, Krista Menard, Laura Monereau, John Morrison, Nirmala Raghavan, Eric E. Shields, Jean Simmermacher-Mayer, Michael Sinz, Ching Kim Tye, Richard Westhouse, Chunshan Xie, Haiying Zhang, Lisa Zhang, Tatyana Zvyaga, Francis Lee, Ashvinikumar V. Gavai, Andrew P. Degnan
Publikováno v:
ACS Medicinal Chemistry Letters. 13:1165-1171
We describe the synthesis of triazole-containing carboline derivatives and their utility as bromodomain and extra-terminal (BET) inhibitors. A convergent synthetic route permitted the detailed investigation of deuteration and fluorination strategies
Autor:
Ching Kim Tye, Chunhong Yan, Sarah C. Traeger, Wayne Vaccaro, Yingru Zhang, Gerry Everlof, Jianqing Li, Henry Yip, Peng Li, John T. Hunt, Michael A. Poss, Gregory D. Vite, Mussari Christopher P, Steven Sheriff, Asoka Ranasinghe, Haiying Zhang, Richard A. Westhouse, Dharmpal S. Dodd, Richard Rampulla, Zheng Yang, Frank Marsilio, Derek J. Norris, Wen-Ching Han, Tram N. Huynh, Yufen Zhao, Patrice Gill, Nirmala Raghavan, Lalgudi S. Harikrishnan, Ashvinikumar V. Gavai, Susan Wee, John S. Tokarski, Dauh-Rurng Wu, Arvind Mathur, Mei-Li Wen, Huiping Zhang, David R. Tortolani, George V. Delucca, Krista Menard, Francis Y. Lee, Claude A. Quesnelle, Dawn Sun, Vijay T. Ahuja, Daniel O'malley, Christine Huang, Muthoni G. Kamau
Publikováno v:
Journal of Medicinal Chemistry. 64:14247-14265
Inhibition of the bromodomain and extra-terminal (BET) family of adaptor proteins is an attractive strategy for targeting transcriptional regulation of key oncogenes, such as c-MYC. Starting with the screening hit 1, a combination of structure-activi
Autor:
Nirmala Raghavan, S. Panboli
Publikováno v:
Indian Journal of Public Health Research & Development. 10:819
Recently, the daily news is overloaded with reports of human atrocities in the society due to the presence of uncontrolled emotions in human life. This is because of high degree of anger and frustration caused by the manifestation of emotional weakne
Autor:
Richard A. Westhouse, Nirmala Raghavan, Donglu Zhang, Weiping Zhao, Alban Allentoff, Ashok Kumar Gupta, W. Griffith Humphreys, Jinping Gan, Guoxiang Shen, Yueping Zhang, Robert M. Borzilleri, Oliver P. Flint, Jonathan L. Josephs, Punit Marathe, Janet Caceres-Cortes, Lifei Wang
Publikováno v:
Chemical Research in Toxicology. 25:556-571
A drug candidate, BMS-A ((N-(4-((1H-pyrrolo[2,3-b]pyridin-4-yl)oxy)-3-fluorophenyl)-1-(4-fluorophenyl) 2-oxo-1,2-dihydropyridine- 3-carboxamide)), was associated with dose- and time-dependent vacuolar degeneration and necrosis of the adrenal cortex f
A low flow ionization technique to integrate quantitative and qualitative small molecule bioanalysis
Publikováno v:
International Journal of Mass Spectrometry. 301:127-135
Mass spectrometry-based assays are used in drug discovery and development to detect, characterize and quantify drugs, metabolites, impurities and degradants. Recently, high resolution-based mass spectrometers have begun to emerge as a platform with p
Autor:
Dauh-Rurng Wu, Zheng Yang, Steven Sheriff, Muthoni G. Kamau, Lalgudi S. Harikrishnan, Dharmpal S. Dodd, Henry Yip, Christine Huang, Yingru Zhang, Yufen Zhao, Jianqing Li, Richard A. Westhouse, Richard Rampulla, Ashvinikumar V. Gavai, Haiying Zhang, Susan Wee, Dawn Sun, Gerry Everlof, Tram N. Huynh, Ching Su, Derek J. Norris, Arvind Mathur, Wayne Vaccaro, Peng Li, Huiping Zhang, Gregory D. Vite, Mussari Christopher P, John T. Hunt, Asoka Ranasinghe, David R. Tortolani, Nirmala Raghavan, Celia D’Arienzo, Daniel O'malley, Vijay T. Ahuja, Patrice Gill, Lisa Zhang, Claude A. Quesnelle, Tokarski John S, Michael A. Poss
Publikováno v:
Cancer Research. 78:5789-5789
Background: The bromodomains and extra-terminal domain (BET) proteins are a family of 4 adapter proteins, BRD2, BRD3, BRD4, and BRDT, that bind to specific acetylated lysine residues on the histone tails of chromatin and recruit additional proteins t
Autor:
Lifei, Wang, Donglu, Zhang, Nirmala, Raghavan, Ming, Yao, Li, Ma, Charles E, Frost, Charles A, Frost, Brad D, Maxwell, Shiang-yuan, Chen, Kan, He, Theunis C, Goosen, W Griffith, Humphreys, Scott J, Grossman
Publikováno v:
Drug Metabolism and Disposition. 38:448-458
Apixaban is an oral, direct, and highly selective factor Xa inhibitor in late-stage clinical development for the prevention and treatment of thromboembolic diseases. The metabolic drug-drug interaction potential of apixaban was evaluated in vitro. Th
Autor:
Kan He, Nirmala Raghavan, Lifei Wang, Robert M. Knabb, Joseph M. Luettgen, W. Griffith Humphreys, Donglu Zhang, Donald J. P. Pinto
Publikováno v:
Drug Metabolism and Disposition. 37:802-808
Apixaban, a potent and highly selective factor Xa inhibitor, is currently under development for treatment of arterial and venous thrombotic diseases. The O-demethyl apixaban sulfate is a major circulating metabolite in humans but circulates at lower
Publikováno v:
Rapid Communications in Mass Spectrometry. 22:109-120
A highly selected reaction monitoring (SRM) method has been investigated for the determination of muraglitazar 1-O-beta-acyl glucuronide in animal and human plasma without chromatographic separation of this naturally formed acyl glucuronide from its
Autor:
Lloyd Lecureux, Samuel J. Bonacorsi, Robert M. Knabb, Kan He, Patrick Y.S. Lam, Mimi Quan, Gary L. Skiles, Laura M. Patrone, Nirmala Raghavan, Haiying Zhang, Shiang-Yuan Chen, Donglu Zhang
Publikováno v:
Drug Metabolism and Disposition. 36:303-315
Razaxaban is a selective, potent, and orally bioavailable inhibitor of coagulation factor Xa. The molecule contains a 1,2-benzisoxazole structure. After oral administration of [(14)C]razaxaban to intact and bile duct-cannulated rats (300 mg/kg) and d