8 Papers
141 Citations
Xin Chen is an academic researcher from Johnson & Johnson Pharmaceutical Research and Development. The author has contributed to research in topics: Protein kinase A & Vascular endothelial growth factor A. The author has an hindex of 8, co-authored 8 publications.
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Papers
Synthesis and Discovery of Macrocyclic Polyoxygenated Bis-7-azaindolylmaleimides as a Novel Series of Potent and Highly Selective Glycogen Synthase Kinase-3β Inhibitors
Gee-Hong Kuo,Catherine Prouty,Alan Deangelis,Lan Shen,David O'neill,Chandra R. Shah,Peter J. Connolly,William V. Murray,Bruce R. Conway,Peter Cheung,Lori Westover,Jun Z. Xu,Richard Look,Keith T. Demarest,Stuart Emanuel,Steven A. Middleton,Linda Jolliffe,Mary Pat Beavers,Xin Chen +18 more
TL;DR: Molecular docking studies were conducted in an attempt to rationalize the GSK-3beta selectivity of azaindolylmaleimides, with mixed results that exhibited little or no inhibitions to a panel of 50 protein kinases.
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Simplified staurosporine analogs as potent JAK3 inhibitors.
Shyh-Ming Yang,Ravi Malaviya,Lawrence J. Wilson,Rochelle L. Argentieri,Xin Chen,Cangming Yang,Bingbing Wang,Druie Cavender,William V. Murray +8 more
TL;DR: The modification led to a new series of simplified staurosporine analogs, which exhibited significant inhibitory activity against Janus kinase 3 (JAK3) and the structure-activity relationships (SAR) are discussed and a proposed binding model is also highlighted.
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Synthesis and Discovery of Pyrazine−Pyridine Biheteroaryl as a Novel Series of Potent Vascular Endothelial Growth Factor Receptor-2 Inhibitors
Gee-Hong Kuo,Aihua Wang,Stuart Emanuel,Alan Deangelis,Rui Zhang,Peter J. Connolly,William V. Murray,Robert H. Gruninger,Jan L. Sechler,Angel R. Fuentes-Pesquera,Dana L. Johnson,Steven A. Middleton,Linda Jolliffe,Xin Chen +13 more
TL;DR: Molecular docking studies were conducted in an attempt to rationalize the unexpected high VEGFR-2 selectivity of 15, which displayed high inhibitory potency on VEGF-stimulated human umbilical vein endothelial cell (HUVEC) proliferation and good selectivity against cell lines such as HUVEC, human aortic smooth muscle cells, and MRC5 lung fibroblasts.
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Synthesis and biological evaluation of novel macrocyclic bis-7-azaindolylmaleimides as potent and highly selective glycogen synthase kinase-3β (GSK-3β) inhibitors☆
Lan Shen,Catherine Prouty,Bruce R. Conway,Lori Westover,Jun Z. Xu,Richard Look,Xin Chen,Mary Pat Beavers,Jerry R. Roberts,William V. Murray,Keith T. Demarest,Gee-Hong Kuo +11 more
TL;DR: The high selectivity, inhibitory potency and cellular activities of these non-crown-ether typed molecules may provide them as a valuable pharmacological tools in elucidating the complex roles of GSK-3β in cell signaling pathways and the potential usage for the treatment of elevated level of G SKS-3 β involved diseases.
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Synthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors.
Gee-Hong Kuo,Catherine Prouty,Aihua Wang,Stuart Emanuel,Alan Deangelis,Yan Zhang,Fengbin Song,Lawrence Beall,Peter J. Connolly,Prahba Karnachi,Xin Chen,Robert H. Gruninger,Jan L. Sechler,Angel R. Fuentes-Pesquera,Steven A. Middleton,Linda Jolliffe,William V. Murray +16 more
TL;DR: The low inhibition of these compounds to the growth of tumor cell lines, such as HeLa, HCT-116, and A375 further confirms that these VEGFR-2 inhibitors are not cytotoxic agents.
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