- AKT3 MODULATORS
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Compounds of Formula Ia, lb, or Ic, Formula (Ia); Formula (Ib); or Formula (Ic), are described, where the various substituents are defined herein. The compounds can modulate a property or effect of Akt3 in vitro or in vivo, and can also be used, individually or in combination with other agents, in the prevention or treatment of a variety of conditions. Methods for synthesizing the compounds are described. Pharmaceutical compositions and methods of using these compounds or compositions, individually or in combination with other agents or compositions, in the prevention or treatment of a variety of conditions are also described.
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Paragraph 0372
(2021/11/13)
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- Structure-activity relationships for 4-anilinoquinoline derivatives as inhibitors of the DNA methyltransferase enzyme DNMT1
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A series of 4-anilinoquinoline derivatives related to the known inhibitor SGI-1027, containing side chains of varying pKa, were prepared by acid-catalysed coupling of the pre-formed side chains with 4-chloroquinolines. The compounds were evaluated for their ability to reduce the level of DNMT1 protein in HCT116 human colon carcinoma cells by Western blotting. With a very strongly basic N-methylpyridinium side chain, only NHCO-linked compounds were effective, whereas less strongly basic ((diaminomethylene)hydrazono)ethyl or 3-methylpyrimidine-2,4-diamine side chains allowed both NHCO- and CONH-linked compounds to show activity. In contrast, the pKa of the quinoline unit had little apparent influence on activity.
- Gamage, Swarna A.,Brooke, Darby G.,Redkar, Sanjeev,Datta, Jharna,Jacob, Samson T.,Denny, William A.
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supporting information
p. 3147 - 3153
(2013/07/05)
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- SAR analysis of a series of acylthiourea derivatives possessing broad-spectrum antiviral activity
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A series of acylthiourea derivatives were designed, synthesized, and evaluated for broad-spectrum antiviral activity with selected viruses from Poxviridae (vaccinia virus) and two different genera of the family Bunyaviridae (Rift Valley fever and La Cross
- Burgeson, James R.,Moore, Amy L.,Boutilier, Jordan K.,Cerruti, Natasha R.,Gharaibeh, Dima N.,Lovejoy, Candace E.,Amberg, Sean M.,Hruby, Dennis E.,Tyavanagimatt, Shanthakumar R.,Allen III, Robert D.,Dai, Dongcheng
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scheme or table
p. 4263 - 4272
(2012/07/17)
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- QUINOLINE DERIVATIVES FOR MODULATING DNA METHYLATION
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Quinoline derivatives, particularly 4-anilinoquinoline derivatives, are provided. Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.
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Page/Page column 55-56
(2008/06/13)
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- Synthetic Applications of N-N Linked Heterocycles. Part 15. A Facile Synthesis of 4-Pyridyl(aryl)amines via the Reaction between 4-Chloro-1-pyridiniopyridinium Salts and Aryl Amines
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4-Chloro-1-pyridiniopyridinium salts (7) and (8) react with primary and secondary arylamines to give high yields of isolable 4-aryliminium salts (9) and (10).These are readily fragmented into 4-pyridyl(aryl)amines (11) and (12) in excellent yields on treatment with sodium cyanide or sodium salts of sulphonic acids.The method fails with the more basic aliphatic amines, since these apparently attack the 2-position of the chloropyridinium ring giving products resulting from ring-opening.Mechanisms of the reactions are discussed.
- Sammes, Michael P.,Ho, King-Wah,Tam, Ming-Lim,Katritzky, Alan R.
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p. 973 - 978
(2007/10/02)
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