Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Fred Konzelmann"'
Autor:
Jin-Jun Liu, Christophe Michoud, Feng Chi, Yang Wen, Qing Xiang, Nam T. Le, Shaoqing Chen, Nicole Jackson, Jian Ping Lou, Li Chen, Chunlin Zhao, Achyutharao Sidduri, Louis Portland, Lyubomir T. Vassilev, Fred Konzelmann, Yingsi Chen, Christian Tovar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2134-2138
A novel series of quinolinyl-methylene-thiazolinones has been identified as potent and selective cyclin-dependent kinase 1 (CDK1) inhibitors. Their synthesis and structure activity relationships (SAR) are described. Representative compounds from this
Autor:
Zhuming Zhang, Melissa Smith, Navita L. Mallalieu, Omar Jose Morales, Kin-Chun Luk, Lee Apostle Mcdermott, Jia K. Li, Tom Flynn, Yi Chen, Brian Higgins, June Ke, Jin-Jun Liu, Hong Yang, Fred Konzelmann, Mary Simcox, Tom Nevins, Thomas Egan, Yingsi Chen, Kenneth Kolinsky, Louise Gerber, Aruna Railkar, Stan Kolis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1950-1953
RO4396686 is a small molecule KDR, FGFR, and PDGFR inhibitor with good pharmacokinetic properties in rodents. In a mouse corneal neovascularization assay, this compound inhibited VEGF-induced angiogenesis. Tested in a H460a xenograft tumor model this
Autor:
Fred Konzelmann, Yingsi Chen, A. Schutt, Hong Yang, Ursula Kammlott, Yi Chen, Mary Simcox, Wanda DePinto, Kin-Chun Luk, Christine Lukacs, Jin-Jun Liu, Apostolos Dermatakis, Xuefeng Yin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:2465-2468
A novel class of 3,5,6-trisubstituted naphthostyril analogues was designed and synthesized to study the structure-activity relationship for inhibition of cyclin-dependent kinase 2 (CDK2). These compounds, particularly molecules with side-chain modifi
Publikováno v:
Tetrahedron Letters. 44:3901-3904
A one-pot synthesis of 3,5,6-trisubstituted naphthostyrils is described. Addition of organometallic reagents to β-iodovinyl ketone 1 followed by elimination gave the Z-form β-alkyl vinyl ketone 15. Intramolecular cyclization of 15 under the reactio
Publikováno v:
Tetrahedron Letters. 44:2545-2548
3-Pyrrolyl-6-fluoro-naphthostyril 13 was synthesized via a base-catalyzed intramolecular cyclization of oxindole precursor 2 (Y=H). Derivatization of 2 (Y=I) through a one-pot reaction give 5-substituted naphthostyrils. This method allows convenient
Autor:
Fred Konzelmann, Harry Allen Albrecht, Chung Chen Wei, G. Beskid, J. G. Christenson, N H Georgopapadakou, Dennis D. Keith, David L. Pruess, K. H. Deitcher
Publikováno v:
Journal of Medicinal Chemistry. 37:400-407
We have previously reported that linking quinolones to the cephalosporin 3'-position through an ester bond, a carbamate function, or a bond through a quaternary nitrogen produced cephalosporins with a dual mode of antibacterial action. We now describ
Autor:
N H Georgopapadakou, Chung Chen Wei, Dennis D. Keith, G. Beskid, J. G. Christenson, Fred Konzelmann, Harry Allen Albrecht, K. H. Deitcher, David L. Pruess
Publikováno v:
ChemInform. 25
We have previously reported that linking quinolones to the cephalosporin 3'-position through an ester bond, a carbamate function, or a bond through a quaternary nitrogen produced cephalosporins with a dual mode of antibacterial action. We now describ
Autor:
Hong Yang, Irena Daniewski, Dorota Miklowski, Brian Higgins, Giacomo Pizzolato, Fred Konzelmann, Christine Lukacs, Peter Michael Wovkulich, Rossman Pamela Loreen, Kenneth Kolinsky, Xuefeng Yin, Wei Chung-Chen, Grace Ju, Qingjie Ding, Kshitij Chhabilbhai Thakkar, Amy Swain, Jin-Jun Liu
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(20)
A novel series of pyrazolobenzodiazepines 3 has been identified as potent inhibitors of cyclin-dependent kinase 2 (CDK2). Their synthesis and structure-activity relationships (SAR) are described. Representative compounds from this class reversibly in