- 2-Guanidinoquinazolines as new inhibitors of the STAT3 pathway
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Synthesis and SAR investigation of 2-guanidinoquinazolines, initially identified in a high content screen for selective STAT3 pathway inhibitors, led to a more potent analog (11c) that demonstrated improved anti-proliferative activity against a panel of HNSCC cell lines.
- Laporte, Matthew G.,Da Paz Lima, Dimas Jos,Zhang, Feng,Sen, Malabika,Grandis, Jennifer R.,Camarco, Daniel,Hua, Yun,Johnston, Paul A.,Lazo, John S.,Resnick, Lynn O.,Wipf, Peter,Huryn, Donna M.
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Read Online
- N-Bu4NI-catalyzed selective dual amination of sp3 C-H bonds: Oxidative domino synthesis of imidazo[1,5-c]quinazolines on a gram-scale
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An n-Bu4NI catalyzed domino reaction that involves selective dual amination of sp3 C-H bonds has been developed. The protocol affords a facile and efficient approach to the synthesis of imidazo[1,5-c] quinazolines under mild conditions.
- Zhao, Dan,Wang, Teng,Shen, Qi,Li, Jian-Xin
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p. 4302 - 4304
(2014/04/17)
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- A novel series of IKKβ inhibitors part I: Initial SAR studies of a HTS hit
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A novel series of (E)-1-((2-(1-methyl-1H-imidazol-5-yl) quinolin-4-yl) methylene) thiosemicarbazides was discovered as potent inhibitors of IKKβ. In this Letter we document our early efforts at optimization of the quinoline core, the imidazole and the semithiocarbazone moiety. Most potency gains came from substitution around the 6- and 7-positions of the quinoline ring. Replacement of the semithiocarbazone with a semicarbazone decreased potency but led to some measurable exposure.
- Cushing, Timothy D.,Baichwal, Vijay,Berry, Karen,Billedeau, Roland,Bordunov, Viola,Broka, Chris,Cardozo, Mario,Cheng, Peng,Clark, David,Dalrymple, Stacie,Degraffenreid, Michael,Gill, Adrian,Hao, Xiaolin,Hawley, Ronald C.,He, Xiao,Jaen, Juan C.,Labadie, Sharada S.,Labelle, Marc,Lehel, Csaba,Lu, Pu-Ping,McIntosh, Joel,Miao, Shichang,Parast, Camran,Shin, Youngsook,Sjogren, Eric B.,Smith, Marie-Louise,Talamas, Francisco X.,Tonn, George,Walker, Keith M.,Walker, Nigel P.C.,Wesche, Holger,Whitehead, Chris,Wright, Matt,Browner, Michelle F.
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scheme or table
p. 417 - 422
(2011/02/28)
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- QUINAZOLINE COMPOUNDS AND THEIR USE IN MCH-RELATED DISEASE
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Compounds of formula (I), are Melanin Concentrating Hormone (MCH) ligands, useful in the treatment of obesity and other MCH-related conditions (I) wherein R1 is: (I) and R2 is CI-, CH3 CF3, or F3C-O-.
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Page/Page column 7
(2008/06/13)
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- Antithrombotic quinoxazolines
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Quinoxazolines having antithrombotic activity. Exemplary of those disclosed are: 4-{[6-(N-carboxymethyl-quinolin-8-yl-sulphonylamino)-1-methyl-2-oxo-1,2-dihydroquinoxalin-3-yl]-methyl}-benzamidine, 4-{[6-(1-(N-cyclopentyl-carboxymethylcarbonylamino)-cyclo-propyl)-1-methyl-2-oxo-1,2-dihydroquinoxalin-3-yl]-methyl}-benzamidine, and 4-{[7-(N-carboxymethylaminocarbonyl-ethylamino)-4-methyl-quinolin-2-yl]-oxo}-benzamidine.
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- Trialkylalanes in palladium-catalyzed C-alkylations of azines
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Carbo-substitution with alkyl groups in halogenoazines is readily effected under the influence of Pd-catalysis with alanes as the donor of the alkyl group. Acta Chemica Scandinavica 1997.
- Lu, Qingbo,Mangalagiu, Lonel,Benneche, Tore,Undheim, Kjell
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p. 302 - 306
(2007/10/03)
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- Trialkylalanes in palladium-catalyzed chemo- and regioselective alkylations
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Carbosubstitution in halogenoazines with alkyl groups is readily effected under the influence of Pd-catalysis with alanes as the donor of the alkyl group.
- Mangalagiu, Ionel,Benneche, Tore,Undheim, Kjell
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p. 1309 - 1312
(2007/10/03)
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- Pyri(mi)dyl-oxy-and -thio-benzoic acid derivatives useful as herbicides and plant growth regulants
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New pyri(mi)dyl-oxy- or -thio-benzoic acid derivatives of the formula STR1 are taught which have herbicidal and plant growth regulating activity. In the formula Z can be Ch or N, X is oxygen or sulphur, A is oxygen, sulphur, a radical R5 --N=or a radical R6 O--N=and B is oxygen, sulphur, a radical STR2 with the proviso that at least one of the radicals R1, R2 or R3 represents alkyl or a part of a 3- to 6-membered fused carbocyclic ring.
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