60813-32-3Relevant academic research and scientific papers
S - Cis Diene Conformation: A New Bathochromic Shift Strategy for Near-Infrared Fluorescence Switchable Dye and the Imaging Applications
Chen, Hsiang-Jung,Chew, Chee Ying,Chang, En-Hao,Tu, Yu-Wei,Wei, Li-Yu,Wu, Bo-Han,Chen, Chien-Hung,Yang, Ya-Ting,Huang, Su-Chin,Chen, Jen-Kun,Chen, I-Chia,Tan, Kui-Thong
supporting information, p. 5224 - 5234 (2018/04/23)
In this paper, we present a novel charge-free fluorescence-switchable near-infrared (IR) dye based on merocyanine for target specific imaging. In contrast to the typical bathochromic shift approach by extending π-conjugation, the bathochromic shift of our merocyanine dye to the near-IR region is due to an unusual S-cis diene conformer. This is the first example where a fluorescent dye adopts the stable S-cis conformation. In addition to the novel bathochromic shift mechanism, the dye exhibits fluorescence-switchable properties in response to polarity and viscosity. By incorporating a protein-specific ligand to the dye, the probes (for SNAP-tag and hCAII proteins) exhibited dramatic fluorescence increase (up to 300-fold) upon binding with its target protein. The large fluorescence enhancement, near-IR absorption/emission, and charge-free scaffold enabled no-wash and site-specific imaging of target proteins in living cells and in vivo with minimum background fluorescence. We believe that our unconventional approach for a near-IR dye with the S-cis diene conformation can lead to new strategies for the design of near-IR dyes.
Synthesis and initial SAR studies of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines: A new class of KDR kinase inhibitors
Fraley, Mark E.,Hoffman, William F.,Rubino, Robert S.,Hungate, Randall W.,Tebben, Andrew J.,Rutledge, Ruth Z.,McFall, Rosemary C.,Huckle, William R.,Kendall, Richard L.,Coll, Kathleen E.,Thomas, Kenneth A.
, p. 2767 - 2770 (2007/10/03)
We have synthesized and evaluated the activity of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines as a new class of KDR kinase inhibitors. Starting with screening lead 1, potency against isolated KDR was fully optimized with 3-thienyl and 4-methoxyphenyl substituents at the 6- and 3-positions (3g, KDR IC50=19 nM), respectively. The synthesis and SAR of these compounds are described.
