- ALPHA, BETA-UNSATURATED AMIDE COMPOUND
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An object of the present invention is to provide an α,β-unsaturated amide compound or a pharmaceutically acceptable salt or the like thereof having anticancer activity and the like. The α,β-unsaturated amide compound represented by the following formula (I) or a pharmaceutically acceptable salt or the like thereof has anticancer activity and the like: [wherein, "A" represents optionally substituted heterocyclic diyl, R1 represents hydrogen atom or optionally substituted lower alkyl, R2 represents optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted aliphatic heterocyclic group or optionally substituted aromatic heterocyclic group, X represents -O-, -S-, -SO2-, -NRX1- (wherein, RX1 represents hydrogen atom or lower alkyl), -CHRX2- (wherein, RX2 represents hydrogen atom or hydroxy), -CH=CH-, -CO- or -NH-CO-, and n1 and n2 are the same or different, and each represents 0 or 1].
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Paragraph 1130
(2020/12/10)
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- Decarboxylative Intramolecular Arene Alkylation Using N-(Acyloxy)phthalimides, an Organic Photocatalyst, and Visible Light
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An intramolecular arene alkylation reaction has been developed using the organic photocatalyst 4CzIPN, visible light, and N-(acyloxy)phthalimides as radical precursors. Reaction conditions were optimized via high-throughput experimentation, and electron-rich and electron-deficient arenes and heteroarenes are viable reaction substrates. This reaction enables access to a diverse set of fused, partially saturated cores which are of high interest in synthetic and medicinal chemistry.
- Sherwood, Trevor C.,Xiao, Hai-Yun,Bhaskar, Roshan G.,Simmons, Eric M.,Zaretsky, Serge,Rauch, Martin P.,Knowles, Robert R.,Dhar, T. G. Murali
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p. 8360 - 8379
(2019/09/03)
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- Mercaptan compound having HDAC6 (histone deacetylase 6) inhibitory activity and application thereof
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The invention belongs to the technical field of medicines and relates to a mercaptan compound having an anti-tumor activity, in particular to a mercaptan compound containing a 6(7)-substituted-N-(6-decylhexyl)-pyrazolo[3,4-e] indazole-3-formamide fragment
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Paragraph 0289; 0290; 0291; 0292
(2019/03/10)
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- a, ? UNSATURATED AMIDE COMPOUND
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The present invention provides an α,β-unsaturated amide compound or a pharmaceutically acceptable salt or the like thereof having anticancer activity and the like represented by the following formula (I): [wherein, "A" represents optionally substituted heterocyclic diyl, R1 represents hydrogen atom or optionally substituted lower alkyl, R2 represents optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted aliphatic heterocyclic group or optionally substituted aromatic heterocyclic group, X represents -O-, -S-, -SO2-, -NRX1- (wherein, RX1 represents hydrogen atom or lower alkyl), -CHRX2- (wherein, RX2 represents hydrogen atom or hydroxy), -CH=CH-, -CO- or -NH-CO-, and n1 and n2 are the same or different, and each represents 0 or 1].
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Paragraph 0943
(2018/11/27)
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- Tandem Oxidative Ring-Opening/Cyclization Reaction in Seconds in Open Atmosphere for the Synthesis of 1-Tetralones in Water-Acetonitrile
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A mild and practical tandem oxidative ring-opening/cyclization reaction mediated by Ce4+ for the synthesis of 1-tetralones is presented. This rapid transformation was completed within 30 s and conducted in an open reactor at 0 °C in a water-acetonitrile mixture. Various cyclobutanol derivatives are transformed into desired products in good to high yields, and this reaction can be easily scaled up to the gram scale.
- Fang, Jingxian,Li, Lesong,Yang, Chu,Chen, Jinping,Deng, Guo-Jun,Gong, Hang
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supporting information
(2018/11/23)
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- Tandem Oxidative Ring-Opening/Cyclization Reaction in Seconds in Open Atmosphere for the Synthesis of 1-Tetralones in Water-Acetonitrile
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A mild and practical tandem oxidative ring-opening/cyclization reaction mediated by Ce4+ for the synthesis of 1-tetralones is presented. This rapid transformation was completed within 30 s and conducted in an open reactor at 0 °C in a water-acetonitrile mixture. Various cyclobutanol derivatives are transformed into desired products in good to high yields, and this reaction can be easily scaled up to the gram scale.
- Fang, Jingxian,Li, Lesong,Yang, Chu,Chen, Jinping,Deng, Guo-Jun,Gong, Hang
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supporting information
p. 7308 - 7311
(2018/11/25)
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- Synthesis and Antiproliferative Activity of Some Ellipticine-Like 11H-Pyrido[a]carbazole Derivatives
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Some modified 11H-pyrido[a]carbazoles (11H-PyC) and their corresponding tetrahydro derivatives (11H-THPyC) were prepared. A common multistep pathway characterized by conventional reactions, including a Fischer-indole-type synthesis, yielded the tetracycli
- Ferlin, Maria Grazia,Gia, Ornella,DallaVia, Lisa
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experimental part
p. 1872 - 1883
(2012/07/03)
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- Synthesis of 3h-quinazolin-4-ones and 4h-3,1-benzoxazin-4-ones via benzylic oxidation and oxidative dehydrogenation using potassium iodide-tert-butyl hydroperoxide
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A simple and elegant method for benzylic activation was demonstrated employing the potassium iodide/tert-butyl hydrogen peroxide catalytic system. This methodology was further extended for the synthesis of biologically important heterocycles namely, 3H-quinazolin-4-ones and 4H-3,1-benzoxazin-4-ones including mecloqualone and etaqualone which are important quinazolinone-based drugs used for the treatment of insomnia in good yields.
- Kumar, R. Arun,Maheswari, C. Uma,Ghantasala, Satheesh,Jyothi,Reddy, K. Rajender
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experimental part
p. 401 - 410
(2011/04/18)
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- (±)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents
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Several amine-substituted 8-amino-5,6,7,8-tetrahydroisoquinolines were examined as conformationally-constrained analogs of the nicotinic cholinergic (nACh) 3-(aminomethyl)pyridines. Although these ligands failed to bind at nACh receptors, the N-ethyl-N-methyl analog 3d was found to be at least equipotent with nicotine in rodent tests of antinociception. The mechanism of action of 3d is currently unknown.
- Dukat, Ma?gorzata,Taroua, Mohamed,Dahdouh, Abdelaziz,Siripurapu, Umamaheswar,Damaj, M. Imad,Martin, Billy R.,Glennon, Richard A.
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p. 3651 - 3654
(2007/10/03)
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- Synthesis, optical resolution, absolute configuration, and preliminary pharmacology of (+)- and (-)-cis-2,3,3a,4,5,9b-hexahydro-1-methyl-1H-pyrrolo- [3,2-h]isoquinoline, a structural analog of nicotine
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Title compound, 8, has been synthesized from isoquinolinone, 1 (an improved preparation for which is presented) and separated into its antipodes with D- and L-di-p-toluoyltartaric acids. These antipodes and the racemic precursor have been evaluated (and found active) in two in vivo systems for their effects. The most potent of the three, (+)-8, has an ED50 of 7.13 μmol/kg for inhibition of spontaneous activity and 7.45 μmol/kg for antinociception compared to 4.44 and 4.81 μmol/kg, respectively, for (S)-(- )-nicotine. Compounds (-)-8 and 7 are about one-fourth as potent. Isomer (+)- 8 has the 3aR,9bS configuration, the latter corresponding to (S)-(-)-nicotine as determined by X-ray crystallography. However, (+)-8 failed to compete for [3H]-nicotine binding, and its pharmacological effects were not blocked by mecamylamine. These bridged nicotine analogs either are binding to an as- yet-unidentified nicotinic receptor or they represent a novel class of non- nicotinic analgesics.
- Glassco,Suchocki,George,Martin,May
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p. 3381 - 3385
(2007/10/02)
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- Synthesis of Arene Oxide and trans-Dihydro Diol Metabolites of Isoquinoline
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5,6-Epoxy-5,6-dihydroisoquinoline 9 and 7,8-epoxy-7,8-dihydroisoquinoline 21 were each obtained by multi-step synthetic sequences from 5,6,7,8-tetrahydroisoquinoline 1.The mammalian metabolite, trans-5,6-dihydroisoquinoline-5,6-diol 10 was chemically synthesised by base-catalysed hydration of the isoquinoline arene oxide 9.
- Boyd, Derek R.,Davies, R. Jeremy H.,Hamilton, Lynne,McCullough, John J.
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- Dopamine Autoreceptor Agonists as Potential Antipsychotics. 3. 6-Propyl-4,5,5a,6,7,8-hexahydrothiazoloquinolin-2-amine
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A series of rigid tricyclic analogues of the dopamine (DA) agonist PD 118440 was synthesized and evaluated for dopaminergic activity and DA autoreceptor selectivity. (R)-(+)-6-Propyl-4,5,5a,6,7,8-hexahydrothiazoloquinolin-2-amine ((+)-6) was identified as the most selective DA autoreceptor agonist from this group of compounds.It inhibited spontaneous locomotor activity (LMA) in rodents, reversed the γ-butyrolactone (GBL) induced accumulation of rat striatal DOPA and inhibited brain DA neuronal firing, all suggestive of direct DA autoreceptor agonist activity.However, (+)-6 is not completely free of postsynaptic DA activity, as evidenced by its stimulation of LMA in rats at high doses and its ability to produce stereotypy.On the other hand, (-)-6 appears to be a weak partial DA agonist with some effects on brain DA synthesis only at high doses.Like other DA autoreceptor agonists and DA antagonists, (+)-6 inhibited Sidman conditioned avoidance in squirrel monkeys, a test predictive of clinical antipsychotic activity.However, unlike classical antipsychotics, (+)-6 did not induce dystonias in haloperidol-sensitized squirrel monkeys, suggesting a minimal propensity toward extrapyramidal side effects (EPS).
- Caprathe, Bradley W.,Jaen, Juan C.,Wise, Lawrence D.,Heffner, Thomas G.,Pugsley, Thomas A.,et al.
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p. 2736 - 2746
(2007/10/02)
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