- An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer
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A number of indole-3-glyoxylamides have previously been reported as tubulin polymerization inhibitors, although none has yet been successfully developed clinically. We report here a new series of related compounds, modified according to a strategy of redu
- Colley, Helen E.,Muthana, Munitta,Danson, Sarah J.,Jackson, Lucinda V.,Brett, Matthew L.,Harrison, Joanne,Coole, Sean F.,Mason, Daniel P.,Jennings, Luke R.,Wong, Melanie,Tulasi, Vamshi,Norman, Dennis,Lockey, Peter M.,Williams, Lynne,Dossetter, Alexander G.,Griffen, Edward J.,Thompson, Mark J.
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p. 9309 - 9333
(2015/12/23)
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- 3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT(1B)) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole
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The synthesis and in vitro and in vivo characteristics of 3-(1,2,5,6-tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one (1, CP-93,129) are described. This rotationally restricted phenolic analogue of RU-24,969 is a potent (15 nM) and selective (200x vs the 5-
- Macor,Burkhart,Heym,Ives,Lebel,Newman,Nielsen,Ryan,Schulz,Torgersen,Koe
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p. 2087 - 2093
(2007/10/02)
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- THE SYNTHESIS OF ROTATIONALY RESTRICTED PHENOLIC ANALOG OF 5-METHOXY-3-(1,2,5,6-TETRAHYDROPYRID-4-YL)INDOLE (RU-24,969)
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Pyrrolopyrid-5-one represents a rotationally restricted phenolic analog of 5-hydroxyindole.The synthesis of the rotationally restricted phenolic analog of the serotonin agonist, 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole (RU-24,969), is prese
- Macor, John E.,Newman, Michael E.
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p. 805 - 809
(2007/10/02)
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- 1-Benzoyl-3-(alkoxy- or alkylthiopyridinyl)ureas
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The present invention is directed to 1-benzoyl-3-(alkoxy- or alkylthiopyridinyl)urea compounds useful as insecticides.
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