Zobrazeno 1 - 10
of 15
pro vyhledávání: '"George V. De Lucca"'
Autor:
Jun Dai, Arvind Mathur, Lihong Cheng, Kim W. McIntyre, Dawn Sun, Joseph A. Tino, Shiuhang Yip, Douglas G. Batt, Jodi K. Muckelbauer, James R. Burke, Joel C. Barrish, Rodney Vickery, Celia D’Arienzo, Luisa Salter-Cid, Qingjie Liu, Tracy L. Taylor, Hua Gong, Mark A. Pattoli, Elizabeth M. Heimrich, Yingru Zhang, Andy J. Tebben, Myra Beaudoin Bertrand, Kathleen M. Gillooly, Chiehying Chang, Percy H. Carter, Scott H. Watterson, Mary T. Obermeier, Claudine Pulicicchio, Aberra Fura, Chunlei Wang, Michael Galella, Charles M. Langevine, Sarah C. Traeger, Lorell Discenza, Peng Li, Yifan Zhang, Qing Shi, Stacey Skala, Dauh-Rurng Wu, Richard Rampulla, George V. De Lucca
Publikováno v:
Journal of Medicinal Chemistry. 59:9173-9200
Bruton's tyrosine kinase (BTK), a nonreceptor tyrosine kinase, is a member of the Tec family of kinases. BTK plays an essential role in B cell receptor (BCR)-mediated signaling as well as Fcγ receptor signaling in monocytes and Fce receptor signalin
Autor:
Alaric J. Dyckman, Joann Strnad, Jodi K. Muckelbauer, Yongmi An, Chiehying Chang, Lin Cheng, Hedy Li, James Lin, Joseph A. Tino, George V. De Lucca, Kim W. McIntyre, Qing Shi, Katerina Leftheris, James R. Burke, Chunjian Liu, Gilbert C. Olini, Andrew J. Tebben, Percy H. Carter, Qian Ruan, S. H. Spergel, Neha Surti
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:2206-2211
Investigation of various heterocyclic core isosteres of imidazopyrazines 1 & 2 yielded purine derivatives 3 & 8 as potent and selective BTK inhibitors. Subsequent SAR studies of the purine series led to the discovery of 20 as a leading compound. Comp
Autor:
Tracy L. Taylor, Douglas G. Batt, Lorell Discenza, ChiehYing J. Chang, Luisa Salter-Cid, Kim W. McIntyre, Myra Beaudoin Bertrand, Percy H. Carter, Yingru Zhang, Qingjie Liu, James R. Burke, Andrew J. Tebben, Zheng Yang, Joel C. Barrish, Rick Rampulla, Aberra Fura, Daniel W. Kukral, Joseph A. Tino, Punit Marathe, Huiping Zhang, Jun Dai, Qing Shi, Arvind Mathur, Kathleen M. Gillooly, Mark A. Pattoli, Mary T. Obermeier, Stacey Skala, Jodi K. Muckelbauer, George V. De Lucca, Rodney Vickery, Celia D’Arienzo
Publikováno v:
Journal of medicinal chemistry. 59(17)
Bruton’s tyrosine kinase (BTK) belongs to the TEC family of nonreceptor tyrosine kinases and plays a critical role in multiple cell types responsible for numerous autoimmune diseases. This article will detail the structure–activity relationships
Autor:
Yang Michael G, Qihong Zhao, Mary Ellen Cvijic, Andrew J. Tebben, Ruowei Mo, George V. De Lucca, Percy H. Carter, Qing Shi, Joel C. Barrish, Robert J. Cherney, Joseph B. Santella, Zili Xiao
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1384-1387
We report the synthesis of 3-phenylsulfonylmethyl cyclohexylaminobenzamides (4) as CCR2 inhibitors for the potential treatment of inflammatory diseases. Several of the compounds display nanomolar binding affinity for CCR2. The in vitro structure–ac
Autor:
Kimberly A. Solomon, Joseph B. Santella, George L. Trainor, Robert C. Newton, Zhang Wang, Dean A. Wacker, George V. De Lucca, Anuk M. Das, Paul Davies, Ui Tae Kim, Maryanne B. Covington, Danielle M. Graden, Gardner Daniel S, Nicole Stowell, Changsheng Zheng, John V. Duncia, Brian J. Vargo, George C. Emmett, Eric A. Wadman, Carl P. Decicco, Patricia K. Welch, Swamy Yeleswaram, Ann Y. Liauw, Soo S. Ko
Publikováno v:
Journal of Medicinal Chemistry. 48:2194-2211
Starting with our previously described(20) class of CC chemokine receptor-3 (CCR3) antagonist, we improved the potency by replacing the phenyl linker of 1 with a cyclohexyl linker and by replacing the 4-benzylpiperidine with a 3-benzylpiperidine. The
Autor:
George L. Trainor, Robert C. Newton, Brian J. Vargo, Carl P. Decicco, Kimberly A. Solomon, Patricia K. Welch, Ui T. Kim, Maryanne B. Covington, Soo S. Ko, Curt Johnson, George V. De Lucca, Paul Davies
Publikováno v:
Journal of Medicinal Chemistry. 45:3794-3804
Structure-activity relationship (SAR) studies of initial screening hits from our corporate library of compounds and a structurally related series of CCR1 receptor antagonists were used to determine that an N-(alkyl)benzylpiperidine is an essential ph
Autor:
George V. De Lucca, Pieter F. W. Stouten, Peter A. Kollman, Ronald M. Klabe, Yong Duan, Lu Wang
Publikováno v:
Journal of Computer-Aided Molecular Design. 15:145-156
The cyclic urea inhibitors of HIV-1 protease generally have two hydroxyl groups on the seven-membered ring. In this study, free energy perturbation and continuum electrostatic calculations were used to study the contributions of the two hydroxyl grou
Autor:
George V. De Lucca
Publikováno v:
The Journal of Organic Chemistry. 63:4755-4766
We have discovered that hexahydro-5,6-dihydroxy-1,3-diazepin-2-ones can undergo a stereospecific, stereoselective-rearrangement, ring-contraction reaction to give the corresponding tetrahydro-5-hyd...
Autor:
George V. De Lucca, Wayne F. Daneker, Paul E. Aldrich, Y. Ru, C.-H. Chang, Charles J. Eyermann, C.Nicholas Hodge, Edward R. Holler, Francis J. Woerner, and Joseph C. Calabrese, Robert F. Kaltenbach, Fernandez Ch, Prabhakar K. Jadhav, Patrick Y.S. Lam, George Emmett
Publikováno v:
Journal of the American Chemical Society. 120:4570-4581
One important factor influencing the affinity of a flexible ligand for a receptor is the internal strain energy required to attain the bound conformation. Calculation of fully equilibrated ensembles of bound and free ligand and receptor conformations
Autor:
George V. De Lucca
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:495-500
Imidazolidinones were synthesized from 7-membered ring cyclic ureas via a sequential series of novel ring contraction reactions proceeding first through the tetrahydropyrimidinones and finally to the 5-membered ring heterocycle. These imidazolidinone