Zobrazeno 1 - 10
of 20
pro vyhledávání: '"David J. Calderwood"'
Autor:
Wilson Noel S, Gagandeep Somal, Michael Z. Hoemann, Don Konopacki, Maria A. Argiriadi, Anil Vasudevan, David B. Duignan, Bruce Clapham, David Banach, Phil B. Cox, Andrew Burchat, David J. Calderwood
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:5562-5567
A series of furano[3,2-d]pyrimidine Syk inhibitors were synthesized and optimized for their enzyme potency and selectivity versus other kinases. In addition, ADME properties were assessed and compounds were prepared with optimized profiles for in viv
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9516261e3731d757da98b64f609b1a0f
https://doi.org/10.1016/j.bmcl.2016.09.077
https://doi.org/10.1016/j.bmcl.2016.09.077
Autor:
Cele Abad-Zapatero, Yong Jia, David J. Burns, Timothy E. Cloutier, Zhili Xin, Douglas Marcotte, Hua Tang, Kenneth M. Comess, Teresa I. Ng, David W. Borhani, Michael L. Coen, Sanyi Wang, Harriet T. Smith, Eric R. Goedken, Danying Song, Jill E. Clampit, Bo Liu, Philip J. Hajduk, Xueheng Cheng, Maria A. Argiriadi, David Banach, Chaohong Sun, Duncan R. Groebe, Elizabeth H. Fry, Christopher Quinn, Gang Liu, David J. Calderwood, Deanna L. Haasch, Vincent S. Stoll, Rebecca J. Gum
Publikováno v:
ACS Chemical Biology. 6:234-244
Inhibition of protein kinases has validated therapeutic utility for cancer, with at least seven kinase inhibitor drugs on the market. Protein kinase inhibition also has significant potential for a variety of other diseases, including diabetes, pain,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b24a8e4dd5ebafebd0f1d8db41a15f68
https://doi.org/10.1021/cb1002619
https://doi.org/10.1021/cb1002619
Autor:
Joanne Kamens, Kristine E. Frank, Xiaolei Zhang, Silvia Kwak, Lu Wang, Denise C. Perron, Biqin Li, Andrew Burchat, David J. Calderwood, Neil Wishart, Richard W. Dixon, Eric F. Johnson, George A. Cunha, Claude Barberis, Maria A. Argiriadi, Christopher M. Harris, Kelly D. Mullen, Xiaoyun Wu, Anna M. Ericsson, Robert V. Talanian, David W. Borhani, Tami R. Zmetra
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:334-337
We describe structure-based optimization of a series of novel 2,4-diaminopyrimidine MK2 inhibitors. Co-crystal structures (see accompanying Letter) demonstrated a unique inhibitor binding mode. Resulting inhibitors had IC50 values as low as 19 nM and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::773564cfc67a4927bdd8f252728b43ba
https://doi.org/10.1016/j.bmcl.2009.10.103
https://doi.org/10.1016/j.bmcl.2009.10.103
Autor:
David J. Calderwood, Wendy Waegell, Michelle Hart, Gavin C. Hirst, Annette Schwartz, Sheldon E. Ratnofsky, Brian Bettencourt, Robert F. Stachlewitz, Tegest Kebede
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 315:36-41
Lck, one of eight members of the Src family of tyrosine kinases, is activated after T cell stimulation and is required for T-cell proliferation and interleukin (IL)-2 production. Inhibition of Lck has been a target to prevent lymphocyte activation an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::41c3e81f6ec872f12ffe0a6183de4445
https://doi.org/10.1124/jpet.105.089169
https://doi.org/10.1124/jpet.105.089169
Autor:
Brad McRae, David W. Borhani, Biqin Li, Kurt Ritter, Gavin C. Hirst, David J. Calderwood, Wendy Waegell, Sheldon E. Ratnofsky, Michael Friedman, A.K.W. Leung
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:2613-2616
We have identified the pyrazolo[3,4-d]pyrimidine A-420983 (compound 7) as a potent inhibitor of lck. A-420983 exhibits oral efficacy in animal models of delayed-type hypersensitivity and organ transplant rejection.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::580da66de5527b2d655e007519b924e5
https://doi.org/10.1016/j.bmcl.2004.02.101
https://doi.org/10.1016/j.bmcl.2004.02.101
Autor:
Andrew Burchat, Michael M. Friedman, David J. Calderwood, Barbara S. Skinner, Kurt Ritter, Gavin C. Hirst, Biqin Li, Paul Rafferty
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:1687-1690
A series of para-substituted 3-phenyl pyrazolopyrimidines was synthesized and evaluated as inhibitors of lck. The nature of the substitution affected enzyme selectivity and potency for lck, src, kdr, and tie-2. The para-phenoxyphenyl analogue 2 is an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::02c10e361ba0df8c865068a299faab12
https://doi.org/10.1016/s0960-894x(02)00196-8
https://doi.org/10.1016/s0960-894x(02)00196-8
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:1683-1686
A series of pyrrolo[2,3-d]pyrimidines was synthesized and evaluated as inhibitors of Lck. Lck accommodates a diverse set of substituents at N-7. Altering the substituent at N-7 provided compound 13, an orally available lck inhibitor which inhibited T
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1d5d34c40184ac8f37749ad47353480f
https://doi.org/10.1016/s0960-894x(02)00195-6
https://doi.org/10.1016/s0960-894x(02)00195-6
Organocerium reactions of benzamides and thiobenzamides: A direct synthesis of tertiary carbinamines
Publikováno v:
Tetrahedron Letters. 38:1241-1244
A simple and efficient process has been developed for the direct conversion of benzamides and thiobenzamides into tertiary carbinamines. A synthesis of benzonitriles from simple benzamides and a thiobenzamide is also described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::22a77985e468ab7def69ccfeaec3be08
https://doi.org/10.1016/s0040-4039(97)00047-6
https://doi.org/10.1016/s0040-4039(97)00047-6
Publikováno v:
ChemInform. 28
A simple and efficient process has been developed for the direct conversion of benzamides and thiobenzamides into tertiary carbinamines. A synthesis of benzonitriles from simple benzamides and a thiobenzamide is also described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3c25ccce6162675c75bc60ab5f026b9e
https://doi.org/10.1002/chin.199723078
https://doi.org/10.1002/chin.199723078
Autor:
Andrew Burchat, Barbara S. Skinner, Gavin C. Hirst, Biqin Li, Paul Rafferty, David J. Calderwood, Michael M. Friedman, Kurt Ritter
Publikováno v:
ChemInform. 33
A series of para-substituted 3-phenyl pyrazolopyrimidines was synthesized and evaluated as inhibitors of lck. The nature of the substitution affected enzyme selectivity and potency for lck, src, kdr, and tie-2. The para-phenoxyphenyl analogue 2 is an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e0054a2bf5375342edb62fa4f9db8d78
https://doi.org/10.1002/chin.200239158
https://doi.org/10.1002/chin.200239158