Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Brian R. Lahue"'
Autor:
Renee L. DesJarlais, Sebastian Salentin, Klavs F. Jensen, Tommi S. Jaakkola, Daniel J. Griffin, Daniel Rodriguez Greve, Li Xing, Richard I. Robinson, Justin S. Cisar, Xinjun Hou, Constantine Kreatsoulas, Jeffrey W. Johannes, Andrew Palmer, Christos A. Nicolaou, Juan C. Alvarez, Regina Barzilay, William H. Green, Thomas J. Struble, Connor W. Coley, Ola Engkvist, Brian R. Lahue, Milan Chytil, Scott P. Brown, Scott Alan Frank, Daniel J. Price, Georg Mogk, Miriam Mathea
Publikováno v:
Journal of Medicinal Chemistry
Artificial intelligence and machine learning have demonstrated their potential role in predictive chemistry and synthetic planning of small molecules; there are at least a few reports of companies employing in silico synthetic planning into their ove
Autor:
Yuan, Tian, Brian R, Lahue, Yao, Ma, Latha G, Nair, Weidong, Pan, Ronald J, Doll, Timothy, Guzi, Yaolin, Wang, Stéphane L, Bogen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 61:128625
The discovery of potent, bioavailable small molecule inhibitors of p53-HDM2 PPI led us to investigate subsequent modifications to address a CYP3A4 time-dependent inhibition liability. On the basis of the crystal structure of HDM2 in complex with 2, f
Autor:
Hakan Gunaydin, Scott A. Johnson, Brian R. Lahue, Blair T. Lapointe, J. Michael Ellis, Michael D. Altman, Peter Fuller
Publikováno v:
ACS Medicinal Chemistry Letters. 9:528-533
[Image: see text] Preclinical optimization of compounds toward viable drug candidates requires an integrated understanding of properties that impact predictions of the clinically efficacious dose. The importance of optimizing half-life, unbound clear
Autor:
Charlie Chang, Zhengwei Peng, Anthony Donofrio, Meir Glick, Scott T. Harrison, Brian R. Lahue
Publikováno v:
Future Medicinal Chemistry. 9:533-536
Autor:
Craig R. Gibeau, Yao Ma, Gerald W. Shipps, Tian Yuan, Brian R. Lahue, Corey Strickland, Stephane L. Bogen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:2735-2738
Led by the structural information of the screening hit with mDM2 protein, a structure modification of Leu26 moiety of the novel p53–hDM2 inhibitors was conducted. A structure–activity relationship study of 4-substituted piperidines revealed compo
Autor:
Yaolin Wang, Yao Ma, Philip Lipari, Stephane L. Bogen, Cynthia Seidel-Dugan, Yinghui Lin, Asra Mirza, Craig R. Gibeau, Doll Ronald J, Corey Strickland, Giovanna Scapin, Winifred W. Prosise, Diane Rindgen, Paul Reichert, Xiaoying Wang, Ming Liu, Brian R. Lahue, Daniel J. Hicklin, Gerald W. Shipps, Tian Yuan, Elise Seigel, Suxing Liu, W. Robert Bishop, Weidong Pan, Amin A. Nomeir, Latha G. Nair
Publikováno v:
ACS Medicinal Chemistry Letters. 7:324-329
A new subseries of substituted piperidines as p53-HDM2 inhibitors exemplified by 21 has been developed from the initial lead 1. Research focused on optimization of a crucial HDM2 Trp23-ligand interaction led to the identification of 2-(trifluoromethy
Autor:
Meir Glick, Brian R. Lahue, Matthew Tudor, Janet Diratsouian, Mary Jo Wildey, Marybeth S. Burton, Robert Mazzola, Scott A. Johnson, Anne Mai Wassermann
Publikováno v:
Bioorganic & Medicinal Chemistry. 28:115192
Identification of purposeful chemical matter on a broad range of drug targets is of high importance to the pharmaceutical industry. However, disease-relevant but more complex hit-finding plans require flexibility regarding the subset of the compounds
Autor:
Gerald W. Shipps, Doll Ronald J, Yao Ma, Latha G. Nair, Stephane L. Bogen, Brian R. Lahue, Weidong Pan, Yaolin Wang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:1983-1986
The discovery of 3,3-disubstituted piperidine 1 as novel p53–HDM2 inhibitors prompted us to implement subsequent SAR follow up directed towards piperidine core modifications. Conformational restrictions and further functionalization of the piperidi
Autor:
Gerald W. Shipps, Brian R. Lahue, Yaolin Wang, Yao Ma, Timothy J. Guzi, Craig R. Gibeau, Zhuyan Guo, Stephane L. Bogen
Publikováno v:
ACS Medicinal Chemistry Letters. 5:572-575
Introduction of an aliphatic side chain to a key position of a novel piperidine-based HDM2 inhibitor scaffold resulted in significant potency gains, enabling further series progression.
Autor:
Manami Shizuka, Margarita Kirova-Snover, Yao Ma, Yaolin Wang, Weidong Pan, Mark A. Miccoy, Brian R. Lahue, Matthew E. Voss, Stephane L. Bogen, Timothy J. Guzi, Latha G. Nair, Yuan Liu, Graig R. Gibeau, Gerald W. Shipps, Tian Yuan, W. Brent Clayton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:1026-1030
The present invention provides a compound of Formula I (The formula should be inserted here) as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also