Zobrazeno 1 - 10
of 42
pro vyhledávání: '"Bradley C, Pearce"'
Autor:
John Morrison, Steven Sheriff, Mark D. Wittman, Gregory A. Locke, Bradley C. Pearce, Erika M. V. Araujo, Andrew P. Degnan, Christopher W. Allard, Dan You, Xin Li, Kurt Zimmermann, Anwar Murtaza, Benjamin M. Johnson, Caitlyn Stromko, Jinqi Liu, Gregory D. Vite, Godwin Kwame Kumi, Karen E. Parrish, Alan Futran, Johnson Walter Lewis
Publikováno v:
ACS Medicinal Chemistry Letters
While the discovery of immune checkpoint inhibitors has led to robust, durable responses in a range of cancers, many patients do not respond to currently available therapeutics. Therefore, an urgent need exists to identify alternative mechanisms to a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe8d6f32c2573a82ac07636c7d82958e
https://doi.org/10.1021/acsmedchemlett.0c00660
https://doi.org/10.1021/acsmedchemlett.0c00660
Autor:
Frank Marsilio, Chiehying Chang, Steven Sheriff, Bradley C. Pearce, Iyoncy Rodrigo, Max Ruzanov, Dasa Lipovsek, Jodi K. Muckelbauer, Mian Gao, Heather Malakian, Dianlin Xie, John A. Newitt, Wai L. Lau
Publikováno v:
Acta Crystallogr F Struct Biol Commun
Hematopoietic progenitor kinase 1 (HPK1) is an intracellular kinase that plays an important role in modulating tumor immune response and thus is an attractive target for drug discovery. Crystallization of the wild-type HPK1 kinase domain has been ham
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bfd023143b3944f7c830323b7394ad11
https://pubmed.ncbi.nlm.nih.gov/33439152
https://pubmed.ncbi.nlm.nih.gov/33439152
Autor:
Hyunsoo Park, James H. Cook, Ivar M. McDonald, Bradley C. Pearce, Matthew D. Hill, Haiquan Fang, John E. Macor, Lizbeth Gallagher, F. Christopher Zusi, Richard E. Olson, Linda J. Bristow
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:5002-5005
We describe an efficient and convergent synthesis of a series of (1'S,2R,4'S)-3H-4'-azaspiro[benzo[4,5]imidazo[2,1-b]oxazole-2,2'-bicyclo[2.2.2]octanes] displaying potency for the α7 nicotinic acetylcholine receptor (nAChR) and good selectivity vs.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::67c17ad27adf8439455974f7b5770b18
https://doi.org/10.1016/j.bmcl.2017.10.009
https://doi.org/10.1016/j.bmcl.2017.10.009
Autor:
Valerie J. Whiterock, Amy Easton, Regina Miller, Lawrence R. Marcin, Meredith Ferrante, Bradley C. Pearce, John B. Hogan, Joanne J. Bronson, Clotilde Bourin, Mendi A. Higgins, Robert G. Gentles, F. Christopher Zusi, Walter Kostich, John E. Macor, Michael Gulianello, Min Ding, Linda J. Bristow, Adam Hendricson, Kim A. Johnson, Andrew Alt, Yanling Huang, Matthew A. Seager
Publikováno v:
Bioorganic & Medicinal Chemistry. 25:496-513
Triazolopyridine ethers with mGlu2 positive allosteric modulator (PAM) activity are disclosed. The synthesis, in vitro activity, and metabolic stability data for a series of analogs is provided. The effort resulted in the discovery of a potent, selec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d4fbbfea4e7fe10fc6e8c858a57219bd
https://doi.org/10.1016/j.bmc.2016.11.018
https://doi.org/10.1016/j.bmc.2016.11.018
Autor:
Zheng Yang, John D. Matiskella, Zhiwei Yin, Zhongxing Zhang, Tao Wang, John F. Kadow, Pin-Fang Lin, Hsu-Tso Ho, Richard J. Colonno, Yasu Ueda, Nicholas A. Meanwell, David R. Langley, Dawn D. Parker, Gregory Yamanaka, Yi-Fei Gong, Ming Zheng, Bradley C. Pearce
Publikováno v:
Journal of medicinal chemistry. 61(14)
The optimization of the 4-methoxy-6-azaindole series of HIV-1 attachment inhibitors (AIs) that originated with 1 to deliver temsavir (3, BMS-626529) is described. The most beneficial increases in potency and pharmacokinetic (PK) properties were attai
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f366c79c2cc59e8a947151d9fef78a24
https://pubmed.ncbi.nlm.nih.gov/29920093
https://pubmed.ncbi.nlm.nih.gov/29920093
Autor:
Arvind Mathur, Rajareddy Kallem, Thaddeus F. Molski, Manjunatha Narayana Rao Kamble, Michelle Nophsker, Huiping Zhang, Murali Subramanian, Dalton King, Linda J. Bristow, Lawrence R. Marcin, B.N. Srikumar, Grandhi Venkat Ram Krishna Mohan Gupta, Kumar Kuchibhotla Vijaya, Jayakumar Sankara Warrier, Michael Sinz, Charulatha Sanmathi, G. Nagaraju, Xiaoliang Zhuo, Raju Mannoori, Imadul Islam, Alicia Ng, Pattipati S. Naidu, Eric Shields, Joanne J. Bronson, Narasimharaju Kalidindi, Reeba K. Vikramadithyan, Gopikishan Tonukunuru, Lorin A. Thompson, James Kempson, Srinivasan Thangathirupathy, Jogi Srinivas, Bradley C. Pearce, Jyoti Gulia, Jean Simmermacher, Srinivas Cheruku, Mahesh Paschapur, Jianliang Shi, John E. Macor, Jayant Aher, Manjunath Ramarao, Charlie F. Albright, Richard E. Olson, Rex Denton, Aliphedi B. Reddy, Hyunsoo Park, Karageorge George N, Tanmaya Bastia, Jianqing Li
Publikováno v:
ACS medicinal chemistry letters. 9(5)
[Image: see text] There is a significant unmet medical need for more efficacious and rapidly acting antidepressants. Toward this end, negative allosteric modulators of the N-methyl-d-aspartate receptor subtype GluN2B have demonstrated encouraging the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::70b5b1329a3adeaa60f04b63eb061394
https://pubmed.ncbi.nlm.nih.gov/29795762
https://pubmed.ncbi.nlm.nih.gov/29795762
Autor:
Min Ding, Hua Fang, Min Gao, Goodrich Jason, Jin-Hua Sun, Bradley C. Pearce, Jeffrey L. Romine, Peter T. Nower, Donald R. O'Boyle, Ying-Kai Wang, Michael H. Serrano-Wu, Lopez Omar D, Lourdes Valera, Lawrence B. Snyder, Rudolph G. Krause, Fukang Yang, Makonen Belema, Denis R. St. Laurent, Xuejie Yang, Nicholas A. Meanwell, Van N. Nguyen, Mengping Liu, Julie A. Lemm
Publikováno v:
Journal of Medicinal Chemistry. 57:1976-1994
A series of symmetrical E-stilbene prolinamides that originated from the library-synthesized lead 3 was studied with respect to HCV genotype 1a (G-1a) and genotype 1b (G-1b) replicon inhibition and selectivity against BVDV and cytotoxicity. SAR emerg
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a899a8f2f22b10fb1c46466cae76e1da
https://doi.org/10.1021/jm301796k
https://doi.org/10.1021/jm301796k
Autor:
Mendi A, Higgins, Lawrence R, Marcin, F, Christopher Zusi, Robert, Gentles, Min, Ding, Bradley C, Pearce, Amy, Easton, Walter A, Kostich, Matthew A, Seager, Clotilde, Bourin, Linda J, Bristow, Kim A, Johnson, Regina, Miller, John, Hogan, Valerie, Whiterock, Michael, Gulianello, Meredith, Ferrante, Yanling, Huang, Adam, Hendricson, Andrew, Alt, John E, Macor, Joanne J, Bronson
Publikováno v:
Bioorganicmedicinal chemistry. 25(2)
Triazolopyridine ethers with mGlu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::c51d8b2216df7c3ae7ce8e46554f0338
https://pubmed.ncbi.nlm.nih.gov/27914948
https://pubmed.ncbi.nlm.nih.gov/27914948
Autor:
Nicholas A, Meanwell, Owen B, Wallace, Haiquan, Fang, Henry, Wang, Milind, Deshpande, Tao, Wang, Zhiwei, Yin, Zhongxing, Zhang, Bradley C, Pearce, Jennifer, James, Kap-Sun, Yeung, Zhilei, Qiu, J J, Kim Wright, Zheng, Yang, Lisa, Zadjura, Donald L, Tweedie, Suresh, Yeola, Fang, Zhao, Sunanda, Ranadive, Brett A, Robinson, Yi-Fei, Gong, Hwei-Gene Heidi, Wang, Timothy P, Spicer, Wade S, Blair, Pei-Yong, Shi, Richard J, Colonno, Pin-Fang, Lin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1977-1981
The effects of introducing simple halogen, alkyl, and alkoxy substituents to the 4, 5, 6 and 7 positions of 1-(4-benzoylpiperazin-1-yl)-2-(1H-indol-3-yl)ethane-1,2-dione, an inhibitor of the interaction between HIV gp120 and host cell CD4 receptors,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2259bba44f301feaba94a75914776769
https://doi.org/10.1016/j.bmcl.2009.02.040
https://doi.org/10.1016/j.bmcl.2009.02.040
Autor:
Eugene V. Genovesi, Yi Zhang, Ashok K. Trehan, Philip R. Wyde, Ivette Medina, Nicholas A. Meanwell, Kathleen F. Kadow, Xiangdong Alan Wang, Rita L. Civiello, Christopher Cianci, Zhiwei Yin, H. Belgin Gulgeze, Keith D. Combrink, Bradley C. Pearce, Junius Clarke, Lucinda Lamb, Kuo-Long Yu, Mark Krystal
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1115-1122
The introduction of acidic and basic functionality into the side chains of respiratory syncytial virus (RSV) fusion inhibitors was examined in an effort to identify compounds suitable for evaluation in vivo in the cotton rat model of RSV infection fo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d1e43e7214e5a9a067bd12b1792d30b1
https://doi.org/10.1016/j.bmcl.2005.11.109
https://doi.org/10.1016/j.bmcl.2005.11.109