- COMPOUNDS AND METHOD OF USE
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This present disclosure relates to compounds with ferroptosis inducing activity, a method of treating a subject with cancer with the compounds, and combination treatments with a second therapeutic agent.
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Paragraph 1209
(2019/09/06)
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- One-pot synthesis of camalexins and 3,3′-biindoles by the Masuda borylation-Suzuki arylation (MBSA) sequence
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The Masuda borylation/Suzuki arylation (MBSA) sequence starting from N-protected 3-iodoindoles has successfully been extended to the coupling of five-membered heterocycles and indoles in the arylation step, which could not be achieved with previously developed MBSA methods. By this approach the one-pot nature of the method as well as the use of a simple catalyst system has been retained. The applicability of the method has been demonstrated by the facile synthesis of camalexins and 3,3′-biindoles, compounds of special interest due to their pronounced antifungal, antimicrobial and cytotoxic activities. The Masuda borylation/Suzuki arylation sequence furnishes in a concise one-pot manner camalexins and 3,3′-biindoles, compounds that show pronounced antifungal, antimicrobial, and cytotoxic activities. Copyright
- Tasch, Boris O. A.,Antovic, Dragutin,Merkul, Eugen,Mueller, Thomas J. J.
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supporting information
p. 4564 - 4569
(2013/07/26)
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- One-pot synthesis of diazine-bridged bisindoles and concise synthesis of the marine alkaloid hyrtinadine A
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Diazine-bridged bisindoles are readily obtained from N-Bocprotected 3-iodoindoles and 3-iodo-7-azaindole in a pseudo three-component reaction involving a one-pot Masuda borylation-Suzuki arylation sequence. Some of the title com-pounds display promising c
- Tasch, Boris O. A.,Merkul, Eugen,Mueller, Thomas J. J.
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supporting information; experimental part
p. 4532 - 4535
(2011/10/03)
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- Design of potent IGF1-R inhibitors related to bis-azaindoles
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From an azaindole lead, identified in high throughput screen, a series of potent bis-azaindole inhibitors of IGF1-R have been synthesized using rational drug design and SAR based on a in silico binding mode hypothesis. Although the resulting compounds produced the expected improved potency, the model was not validated by the co-crystallization experiments with IGF1-R.
- Nemecek, Conception,Metz, William A.,Wentzler, Sylvie,Ding, Fa-Xiang,Venot, Corinne,Souaille, Catherine,Dagallier, Anne,Maignan, Sebastien,Guilloteau, Jean-Pierre,Bernard, Francois,Henry, Alain,Grapinet, Sandrine,Lesuisse, Dominique
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scheme or table
p. 100 - 106
(2011/03/19)
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- Amino-zinc-ene-enolate cyclization: A short access to cis-3-substituted prolino-homotryptophane derivatives
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(Chemical Equation Presented) Proline chimeras are useful tools for medicinal chemistry and/or biological applications. The asymmetric synthesis of cis-3-substituted prolines can be easily achieved via amino-zinc-ene-enolate cyclization followed by transm
- Mothes, Celine,Lavielle, Solange,Karoyan, Philippe
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p. 6706 - 6710
(2008/12/22)
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- Hydroboration and Suzuki-Miyaura coupling reactions with the electronically modulated variant of an ynamine: The synthesis of (E)-β-arylenamides
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The first hydroboration of an 1-alkynylamide - the electronically modulated variant of an ynamine - is described. This hydroboration in combination with a Suzuki-Miyaura cross-coupling reaction with aryl bromides or aryl iodides allows a flexible synthesis of (E)-β-arylenamides and 3-(2'-amidovinyl)indoles with high degree of molecular diversity. (C) 2000 Elsevier Science Ltd.
- Witulski, Bernhard,Buschmann, Nicole,Bergstr??er, Uwe
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p. 8473 - 8480
(2007/10/03)
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- Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase. 6. 2-Indol-3-yl- and 2-azaindol-3-yl- dipyridodiazepinones
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Modification of the non-nucleoside inhibitor of HIV-1 reverse transcriptase nevirapine (Viramune) by incorporation of a 2-indolyl substituent confers activity against several mutant forms of the enzyme.
- Kelly,McNeil,Rose,David,Shih,Grob
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p. 2430 - 2433
(2007/10/03)
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