- Design, synthesis, biological evaluation, and Structure - Activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4
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Sixty-one phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates (PIB-SOs) and 13 of their tetrahydro-2-oxopyrimidin-1(2H)-yl analogues (PPB-SOs) were prepared and biologically evaluated. The antiproliferative activities of PIB-SOs on 16 cancer cell lines are
- Fortin, Sébastien,Wei, Lianhu,Moreau, Emmanuel,Lacroix, Jacques,C?té, Marie-France,Petitclerc, éric,Kotra, Lakshmi P.,C.-Gaudreault, René
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experimental part
p. 4559 - 4580
(2011/09/15)
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- SUBSTITUTED 2-IMIDAZOLIDONES AND ANALOGS
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Compounds of formula (I): wherein R1, R2, R3, R4, R7, R6, R7, R8, R9, A, X and Y as defined herein are provided as useful for the treatment of cancer or for
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Page/Page column 85
(2011/09/19)
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- COMPOUNDS AND METHODS FOR TREATING INFLAMMATORY AND FIBROTIC DISORDERS
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Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
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Page/Page column 86
(2009/12/28)
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- Cyclic ureas as ortho directing substituents
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Six-membered cyclic ureas are shown to have a weak ortho directing ability when linked through nitrogen to benzene and pyridine rings.
- Meigh,Alvarez,Joule
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p. 2012 - 2021
(2007/10/03)
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- New substituted 1-(2,3-dihydrobenzo[1,4]dioxin-2-ylmethyl)piperidin-4-yl derivatives with α2-adrenoceptor antagonist activity
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The emergence of a novel theory concerning the role of noradrenaline in the progression and the treatment of neurodegenerative diseases such as Parkinson's and Alzheimer's diseases has provided a new impetus toward the discovery of novel compounds acting at α2-adrenoceptors. A series of substituted 1-(2,3-dihydrobenzo[1,4]dioxin-2-ylmethyl)piperidin-4-yl derivatives bearing an amide, urea, or imidazolidinone moiety was studied. Some members of this series of compounds proved to be potent α2-adrenoceptor antagonists with good selectivity versus α1-adrenergic and D2-dopamine receptors. Particular emphasis is given to compound 33g which displays potent α2-adrenoceptor binding affinity in vitro and central effects in vivo following oral administration.
- Mayer,Brunel,Chaplain,Piedecoq,Calmel,Schambel,Chopin,Wurch,Pauwels,Marien,Vidaluc,Imbert
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p. 3653 - 3664
(2007/10/03)
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- 3-(piperid-4-yl)-1,2-benzisoxazole and 3-(piperazin-4-yl)-1,2-benzisoxazole compounds
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Compounds of formula: STR1 wherein: A, m, n, E and Y are as defined in the description, the optical isomers thereof and the physiologically-tolerable salts thereof. These compounds, their optical isomers and their physiologically-tolerable salts, can be u
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- sYNTHESIS OF N,N'-DISUBSTITUTED UREAS FROM CARBAMATES
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A simple synthesis of N,N'-disubstituted ureas from carbamates is described involving displacement of an alkoxy group by the magnesium salt of an amine generated in situ by treatment with ethylmagnesium bromide.
- Basha, Anwer
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p. 2525 - 2526
(2007/10/02)
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- Controlled Reduction of Pyrimidin(e)-2(1H)-ones and -thiones with Metal Hydride Complexes. Regioselective Preparation of Dihydro- and Tetrahydro-pyrimidin-2(1H)-ones and the Corresponding Thiones
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1,4,6-Trisubstituted pyrimidin-2(1H)-ones were easily reduced with sodium borohydride to give mixtures of 3-aryl-3,4-dihydro-, 1-aryl-3,4-dihydro-, and 3,4,5,6-tetrahydro-pyrimidin-2(1H)-ones.The ratio of the three products was dramatically dependent on t
- Kashima, Choji,Katoh, Akira,Yokota, Yuko,Omote, Yoshimori
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p. 1622 - 1625
(2007/10/02)
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