61640-21-9Relevant academic research and scientific papers
Platinum-catalyzed domino reaction with benziodoxole reagents for accessing benzene-alkynylated Indoles
Li, Yifan,Waser, Jerome
, p. 5438 - 5442 (2015/04/27)
Indoles are omnipresent in natural products, bioactive molecules, and organic materials. Consequently, their synthesis or functionalization are important fields of research in organic chemistry. Most works focus on installation or modification of the pyrrole ring. To access benzene-ring-functionalized indoles with an unsubstituted pyrrole ring remains more challenging. Reported herein is a platinum-catalyzed cyclization/alkynylation domino process to selectively obtain C5- or C6-functionalized indoles starting from easily available pyrroles. The work combines, for the first time, a platinum catalyst with ethynylbenziodoxole hypervalent iodine reagents in a domino process for the synthesis of polyfunctionalized arene rings and gives access to important building blocks for the synthesis of bioactive compounds and organic materials.
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[ b ]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties
Flynn, Bernard L.,Gill, Gurmit S.,Grobelny, Damian W.,Chaplin, Jason H.,Paul, Dharam,Leske, Annabell F.,Lavranos, Tina C.,Chalmers, David K.,Charman, Susan A.,Kostewicz, Edmund,Shackleford, David M.,Morizzi, Julia,Hamel, Ernest,Jung, M. Katherine,Kremmidiotis, Gabriel
, p. 6014 - 6027 (2011/10/31)
A structure-activity relationship (SAR) guided design of novel tubulin polymerization inhibitors has resulted in a series of benzo[b]furans with exceptional potency toward cancer cells and activated endothelial cells. The potency of early lead compounds has been substantially improved through the synergistic effect of introducing a conformational bias and additional hydrogen bond donor to the pharmacophore. Screening of a focused library of potent tubulin polymerization inhibitors for selectivity against cancer cells and activated endothelial cells over quiescent endothelial cells has afforded 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105, 8) as a potent and selective antiproliferative. Because of poor solubility, 8 is administered as its disodium phosphate ester prodrug 9 (BNC105P), which is rapidly cleaved in vivo to return the active 8. 9 exhibits both superior vascular disrupting and tumor growth inhibitory properties compared with the benchmark agent combretastatin A-4 disodium phosphate 5 (CA4P).
Formation of stable neutral copper bis-dithiolene thin films by potentiostatic electrodeposition
Dalgleish, Simon,Awaga, Kunio,Robertson, Neil
supporting information; experimental part, p. 7089 - 7091 (2011/08/06)
Thin films of neutral copper dithiolenes have been prepared by potentiostatic electrodeposition. This method allows the isolation of near infrared (NIR) active species, in a useable form, that are otherwise unobtainable by conventional chemical methods.
Indole-substituted nickel dithiolene complexes in electronic and optoelectronic devices
Dalgleish, Simon,Labram, John G.,Li, Zhe,Wang, Jianpu,McNeill, Christopher R.,Anthopoulos, Thomas D.,Greenham, Neil C.,Robertson, Neil
experimental part, p. 15422 - 15430 (2012/01/14)
The synthesis and full characterisation of a novel indole-substituted nickel dithiolene [Ni(mi-5edt)2] (3) is reported, and compared to its alkyl-substituted analogue [Ni(mi-5hdt)2] (4) that has been previously communicated [Dalgleish et al., Chem. Commun., 2009, 5826] [mi-5edt = 1-(N-methylindol-5-yl)-ethene-1,2-dithiolate; mi-5hdt = 1-(N-methylindol-5-yl)- hex-1-ene-1,2-dithiolate)]. Both complexes are shown to undergo oxidative electropolymerisation, yielding polymer films that retain the redox and optical properties of the monomer. The more soluble analogue 4 is shown to form high quality thin films by spin coating, which have been utilised to fabricate field-effect transistors (FETs) and bulk heterojunction photovoltaic devices (BHJ-PVs). From FET studies, the material shows ambipolar charge transport behaviour, with a maximum carrier mobility of ～10-6 cm 2 V-1 s-1 for electrons. By using 4 simultaneously as the electron acceptor as well as a NIR sensitiser in BHJ-PVs, the complex is shown to contribute to the photocurrent, extending light harvesting into the NIR region.
CHEMICAL COMPOUNDS AND PROCESSES
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Page/Page column 55; 56, (2008/12/06)
The present invention relates generally to chemical compounds and methods for their use and preparation. In particular, the invention relates to chemical compounds which may possess useful therapeutic activity, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds.
