Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Jane L. Holmes"'
Autor:
Tieguang Yao, Liangwei Wu, Craig S. Donald, Douglas Ferguson, Lei Wang, Andrew Pike, Jianyan Wang, Justin Cidado, Dedong Wu, Kurt Gordon Pike, Kumar Thakur, Chungang Gu, Calum Cook, James Horstick, Tyler Grebe, Theresa Proia, Darren Stead, Alexander Hird, Michelle Lamb, Wenlin Shao, Nichole O'Connell, Yun Jiang, Sudhir M. Hande, Bin Yang, Janet Hawkins, Barlaam Bernard Christophe, Neil Sumner, Melissa Vasbinder, Andrew D. Ferguson, Jane E. Moore, Jeffrey G. Varnes, Bryan Roberts, Maryann San Martin, Lisa Drew, Ujjal Sarkar, Allan Dishington, Chris De Savi, Robert Casella, Steve C. Glossop, Jane L. Holmes, Thomas M. McGuire
Publikováno v:
Journal of Medicinal Chemistry. 63:15564-15590
A CDK9 inhibitor having short target engagement would enable a reduction of Mcl-1 activity, resulting in apoptosis in cancer cells dependent on Mcl-1 for survival. We report the optimization of a series of amidopyridines (from compound 2), focusing o
Autor:
Lei Wang, Allan Dishington, Jane E. Moore, Kurt Gordon Pike, Wenlin Shao, Andrew Lister, Anil Patel, Lorraine A. Hassall, Sudhir M. Hande, Jane L. Holmes, Douglas Ferguson, Thomas M. McGuire, Jeffrey G. Varnes, Lin Xue, Chungang Gu, Tieguang Yao, Barlaam Bernard Christophe, Lisa Drew, Janet Hawkins, Liangwei Wu, Chris De Savi, Melissa Vasbinder, Andrew D. Ferguson, Darren Stead, Ujjal Sarkar, Michelle Lamb, Nichole O'Connell, Bin Yang, Alexander Hird
Publikováno v:
Journal of medicinal chemistry. 64(20)
Optimization of a series of azabenzimidazoles identified from screening hit 2 and the information gained from a co-crystal structure of the azabenzimidazole-based lead 6 bound to CDK9 led to the discovery of azaindoles as highly potent and selective
Autor:
Camila de-Almeida, Keith R. Mulholland, Kang Zhao, Barlaam Bernard Christophe, Gilles Ouvry, Gareth Hughes, Martin Pass, Elaine Cadogan, Zhenhua Wang, Andrew D. Campbell, Nidal Al-Huniti, Natalie Stratton, Sébastien L. Degorce, Joanne Wilson, Myriam Didelot, Philip A. MacFaul, Stephen T. Durant, Richard Ducray, Baochang Zhai, Kurt Gordon Pike, Lorraine A. Hassall, Jane L. Holmes, Thomas M. McGuire, Nichola L. Davies, Allan Dishington, Yingxue Chen, Nicola Colclough, Graeme R. Robb
Publikováno v:
Journal of Medicinal Chemistry. 61:3823-3841
ATM inhibitors, such as 7, have demonstrated the antitumor potential of ATM inhibition when combined with DNA double-strand break-inducing agents in mouse xenograft models. However, the properties of 7 result in a relatively high predicted clinically
Autor:
Anil Patel, Rebecca E. Meadows, Kurt Gordon Pike, Jane E. Moore, Turner Paul, Darren Stead, Barlaam Bernard Christophe, Andrew Stark, Jemma Clark, Janet Hawkins, Bin Yang, Bryan Roberts, Craig S. Donald, Gemma Davison, Esther Moore, Chris De Savi, Tyler Grebe, Calum Cook, Melissa Vasbinder, Simon C. C. Lucas, Andrew Lister, Jeffrey G. Varnes, Kumar Thakur, Sudhir M. Hande, Jane L. Holmes, Thomas M. McGuire, Alexander Hird, Allan Dishington
Publikováno v:
Tetrahedron Letters. 57:4718-4722
As part of a medicinal chemistry program, we adapted known synthetic methods for the late-stage diversification of 2,4-substituted 7-azaindoles. The strengths and weaknesses of these strategies are discussed. In the course of this work, three optimiz
Autor:
Laksmaiah Gingipalli, Jane E. Moore, Rosemary A. Croft, Barlaam Bernard Christophe, Janet Hawkins, Hai-Jun Zhang, Tao Wang, Anil Patel, Lynsie Almeida, Xiaolan Zheng, Kurt Gordon Pike, Timothy Pontz, Allan Dishington, Stephanos Ioannidis, Xiaoyun Wu, Jeffrey W. Johannes, Lorraine A. Hassall, Jane L. Holmes, Thomas M. McGuire
Publikováno v:
Synthesis. 48:1226-1234
Examples of hydroxymethylated analogues of heteroaryl cores such as quinazolin-4-ones, isoquinolin-1(2H)-ones, pyrido[3,4-d]pyrimidin-4(3H)-ones, chromen-4-ones and pyrrolo[2,1-f][1,2,4]triazin-4(3H)-ones are sparse or non-existent in the scientific
Publikováno v:
Tetrahedron Letters. 55:6734-6737
A synthetic strategy for the synthesis of a library of 4- N -benzylamino-2- N -phenyl-pyridines is herein described. The approach involves a Pd-assisted cross-coupling of a 4-chloro- N -phenylpyridin-2-amine intermediate with a range of benzylamines.
Autor:
Suzanne S. Bowker, Clive Green, Graeme R. Robb, Stephen Stokes, Nathaniel G. Martin, Anne Ertan, David G.A. Morgan, Christopher Sheldon, Alexander G. Dossetter, Robert D. M. Davies, David S. Clarke, Alastair J. H. Brown, William McCoull, Helen Pointon, Jane E. Moore, Mark L. Fenwick, Nicholas John Newcombe, Claire Newton, Jane L. Holmes, David J. Masters, Peter Barton, Jennifer Cameron
Publikováno v:
Journal of Medicinal Chemistry. 57:6128-6140
Ghrelin plays a major physiological role in the control of food intake, and inverse agonists of the ghrelin receptor (GHS-R1a) are widely considered to offer utility as antiobesity agents by lowering the set-point for hunger between meals. We identif
Autor:
Jane L. Holmes, null et al.
Publikováno v:
ChemInform. 47
Publikováno v:
ChemInform. 46
Autor:
Graeme R. Robb, Lynsie Almeida, Rosemary A. Croft, Jian Huang, Haiyun Wang, Chungang Gu, Jane E. Moore, Steven L. Kazmirski, Michelle Lamb, Nancy Su, Timothy Pontz, Kurt Gordon Pike, Robert Casella, Hai-Jun Zhang, Xiaoyun Wu, Lakshmaiah Gingipalli, Derek Ogg, Barlaam Bernard Christophe, Janet Hawkins, Jeffrey W. Johannes, P. Ann Boriack-Sjodin, Allan Dishington, Yue Zhang, Stephanos Ioannidis, Tina Howard, Xiaolan Zheng, Tao Wang, Anil Patel, Jane L. Holmes, Thomas M. McGuire
Publikováno v:
ACS medicinal chemistry letters. 6(3)
The canonical Wnt pathway plays an important role in embryonic development, adult tissue homeostasis, and cancer. Germline mutations of several Wnt pathway components, such as Axin, APC, and ß-catenin, can lead to oncogenesis. Inhibition of the poly