作者:Mark R Fielding、Ronald Grigg、Visuvanathar Sridharan、Mark Thornton-Pett、Christopher J Urch
DOI:10.1016/s0040-4020(01)00740-2
日期:2001.9
Katritzky's oxopyridinium. betaine cycloaddition is employed to generate bridged bicyclic substrates suitable for our palladium(0) catalysed cyclisation-anion capture methodology. A variety of polycyclic heterocycles have been synthesised via monocyclisation-organotin(IV) capture with or without incorporation of carbon monoxide. Sequential cycloaddition-cyclisation can be performed as a one pot process to deliver substantial gain in molecular complexity. (C) 2001 Elsevier Science Ltd. All rights reserved.
Molecular receptors for monosaccharides: di(pyridyl)naphthyridine and di(quinolyl)naphthyridine
The recognition capabilities of two molecular receptors 2,7-di(3'-pyridyl)-1,8-naphthyridine (DPN) and 2,7-di(3'-quinolyl)-1,8-naphthyridine (DQN) toward monosaccharides in chloroform were evaluated. Both DPN and DQN possess a naphthyridine core moiety, in which two pyridinic nitrogen atoms serve as the proton acceptors. Attached to the C2 and C7 positions of naphthyridine are two identical arms, each of which consists of pyridine (DPN) or quinoline (DQN) moiety that also acts as the proton acceptor. The arrangement of hydroxyl groups in monosaccharides offers the proton donors complementary to the proton acceptors of DPN (or DQN) to form a quadruply hydrogen bonds complex. The binding processes were studied by UV-vis, fluorescence and H-1 NMR spectrophotometric titrations as well as electrospray ionization mass spectroscopy. The binding strength between DPN (or DQN) and examined monosaccharides was comparable to that for man other hydrogen-bonding host molecules previously reported. (c) 2005 Elsevier Ltd. All rights reserved.
A versatile new synthesis of 4-aryl- and heteroaryl-[3,4-c]pyrrolocarbazoles by [4+2] cycloaddition followed by palladium catalysed cross coupling
4-Bromo- and 4-trifluorosulfonyloxypyrrolo[3,4-c]carbazoles were prepared in five steps via a [4+2] cycloaddition and were used as key intermediates in palladium-catalysed cross coupling reactions allowing the rapid generation of structurally diverse protein kinase C inhibitors. (C) 1999 Published by Elsevier Science Ltd. All rights reserved.
Discovery of 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines as potent PIM inhibitors
作者:Bin Wu、Hui-Ling Wang、Victor J. Cee、Brian A. Lanman、Thomas Nixey、Liping Pettus、Anthony B. Reed、Ryan P. Wurz、Nadia Guerrero、Christine Sastri、Jeff Winston、J. Russell Lipford、Matthew R. Lee、Christopher Mohr、Kristin L. Andrews、Andrew S. Tasker
DOI:10.1016/j.bmcl.2014.12.091
日期:2015.2
PIM kinases are a family of Ser/Thr kinases that are implicated in tumorigenesis. The discovery of a new class of PIM inhibitors, 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines, is discussed with optimized compounds showing excellent potency against all three PIM isoforms. (C) 2015 Elsevier Ltd. All rights reserved.
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