439811-16-2Relevant academic research and scientific papers
Structure and activity relationships of tartrate-based TACE inhibitors
Li, Dansu,Popovici-Muller, Janeta,Belanger, David B.,Caldwell, John,Dai, Chaoyang,David, Maria,Girijavallabhan, Vinay M.,Lavey, Brian J.,Lee, Joe F.,Liu, Zhidan,Mazzola, Rob,Rizvi, Razia,Rosner, Kristin E.,Shankar, Bandarpalle,Spitler, Jim,Ting, Pauline C.,Vaccaro, Henry,Yu, Wensheng,Zhou, Guowei,Zhu, Zhaoning,Niu, Xiaoda,Sun, Jing,Guo, Zhuyan,Orth, Peter,Chen, Shiying,Kozlowski, Joseph A.,Lundell, Daniel J.,Madison, Vincent,McKittrick, Brian,Piwinski, John J.,Shih, Neng-Yang,Shipps Jr., Gerald W.,Siddiqui, M. Arshad,Strickland, Corey O.
, p. 4812 - 4815 (2010)
The syntheses and structure-activity relationships of the tartrate-based TACE inhibitors are discussed. The optimization of both the prime and non-prime sites led to compounds with picomolar activity. Several analogs demonstrated good rat pharmacokinetics
Tuning the Circular Dichroism and Circular Polarized Luminescence Intensities of Chiral 2D Hybrid Organic–Inorganic Perovskites through Halogenation of the Organic Ions
Chao, Yu-Chiang,Chen, Deng-Gao,Chiu, Ching-Wen,Chou, Pi-Tai,Lin, Jin-Tai,Lin, Tai-Chun,Liu, Yi-Hung,Yang, Lan-Sheng
, p. 21434 - 21440 (2021/08/20)
Through the incorporation of various halogen-substituted chiral organic cations, the effects of chiral molecules on the chiroptical properties of hybrid organic–inorganic perovskites (HOIPs) are investigated. Among them, the HOIP having a Cl-substituted chiral cation exhibits the highest circular dichroism (CD) and circular polarized luminescence (CPL) intensities, indicating the existence of the largest rotatory strength, whereas the F-substituted HIOP shows the weakest intensities. The observed modulation can be correlated to the varied magnetic transition dipole of HOIPs, which is sensitive to the d-spacing between inorganic layers and the halogen–halogen interaction between organic cations and the inorganic sheets. These counteracting effects meet the optimal CD and CPL intensity with chlorine substitution, rendering the rotatory strength of HOIPs arranged in the order of (ClMBA)2PbI4>(BrMBA)2PbI4>(IMBA)2PbI4>(MBA)2PbI4>(FMBA)2PbI4.
Radiopharmaceutical products for diagnosis and therapy of renal carcinoma
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Paragraph 0058-0060, (2014/05/06)
A radiopharmaceutical composition is disclosed comprising novel iodometomidate derivatives of formula (I) which bind specifically to adrenal enzymes and which exhibit an improved stability. The compounds of formula (I) are suitable for use in a diagnostic
RADIOPHARMACEUTICAL PRODUCTS FOR DIAGNOSIS AND THERAPY OF ADRENAL CARCINOMA
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Page/Page column 14; 15, (2014/04/17)
A radiopharmaceutical composition is disclosed comprising novel iodometomidate derivatives of formula (I) which bind specifically to adrenal enzymes and which exhibit an improved stability. The compounds of formula (I) are suitable for use in a diagnostic
Discovery of novel sphingosine kinase-1 inhibitors. Part 2
Xiang, Yibin,Hirth, Bradford,Kane Jr., John L.,Liao, Junkai,Noson, Kevin D.,Yee, Christopher,Asmussen, Gary,Fitzgerald, Maria,Klaus, Christine,Booker, Michael
scheme or table, p. 4550 - 4554 (2010/09/14)
Building on our initial work, we have identified additional novel inhibitors of sphingosine kinase-1 (SK1). These new analogs address the shortcomings found in our previously reported compounds. Inhibitors 51 and 54 demonstrated oral bioavailability in a
Discovery of melanin-concentrating hormone receptor R1 antagonists using high-throughput synthesis
Su, Jing,McKittrick, Brian A.,Tang, Haiqun,Czarniecki, Michael,Greenlee, William J.,Hawes, Brian E.,O'Neill, Kim
, p. 1829 - 1836 (2008/02/02)
A structure-activity study on benzylpiperidine 1 was accomplished by utilizing high-throughput synthesis. Three focused libraries were designed and synthesized to quickly develop SAR. Further optimization led to the discovery of compound 2, an MCH receptor R1 antagonist with over 400-fold improvement in biological activity over the original lead.
