- NOVEL COMPOUNDS AS INHIBITORS OF DNA METHYLTRANSFERASES
-
It relates to the compounds of formula (I), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures thereof, wherein A, R1, R2, and R3 are as defined herein, which are inhibitors of one or more DNMTs selected from the group consisting of DNMT1, DNMT3A and DNMT3B. It also relates to pharmaceutical or veterinary compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of cancer, fibrosis and/or immunomodulation.
- -
-
Page/Page column 55
(2017/08/01)
-
- Studies on synthesis of a novel, broad-spectrum antitumor compound 2-(1-hydroxy-4-oxo-cyclohexa-2, 5-dienyl)-pyran-4-one
-
Based on the previous studies, used protoapigenone as a model, we adopted chemical synthesis methods to develop the new compounds. It was specifically named as 2-(1-hydroxy-4-oxo-2, 5-cyclohexadien-1-yl)-4H-Pyran-4-one, including a core group: 1-hydroxycy
- Wang, Xiaohua,Yang, Liu,Xue, Pingping,Ruan, Jinlan
-
-
- Henry reaction of fluorinated nitro compounds
-
The Henry (nitroaldol) reaction of fluorinated nitro compounds with various aromatic aldehydes and a fluorinated aliphatic aldehyde to give β-fluoro-β-nitroalcohols which bearing a fluorinated quaternary carbon center was reported. The relative configuration of the major diastereoisomer of 2-fluoro-2-nitro-1-(4-nitrophenyl)-3-phenylpropanol (5bf) was determined by X-ray single crystal analysis.
- Hu, Huawei,Huang, Yangen,Guo, Yong
-
experimental part
p. 108 - 114
(2012/02/05)
-
- A novel, broad-spectrum antitumor compound containing the 1-hydroxycyclohexa-2,5-dien-4-one group: The disclosure of a new antitumor pharmacophore in protoapigenone 1
-
The synthesis of a new compound 9 containing the 4-hydroxy-2,5- cyclohexadien-1-one system, a key elements toward elucidation of the protoapigenone 1 antitumor pharmacophore, was described. The compound showed potent in vitro antitumor potency with low mi
- Yuan, Qianying,Liu, Ziwei,Xiong, Chaomei,Wu, Liqian,Wang, Jianping,Ruan, Jinlan
-
scheme or table
p. 3427 - 3430
(2011/07/07)
-
- METHODS FOR THE PREPARATION OF PYRAZOLE-CONTAINING COMPOUNDS
-
The present invention is directed to novel processes for the preparation of fused pyrazole compounds, useful for the treatment of disorders and conditions mediated by serotonin receptor activity.
- -
-
Page/Page column 13
(2008/06/13)
-
- On the Scope of Asymmetric Nitrile Oxide Cycloadditions with Oppolzer's Chiral Sultam. Total Syntheses of (+)-Hepialone, (-)-(1R,3R,5S)-1,3-Dimethyl-2,9-dioxabicyclooctane
-
Cycloadditions of nitrile oxides with acryloyl derivatives of Oppolzer's chiral sultam produce stereoisomeric Δ2-isoxazolines in ratios of about 90/10 at 25 deg C.The major diastereomers can be isolated in pure form in 70-88percent yield.Synthe
- Curran, Dennis P.,Heffner, Timothy A.
-
p. 4585 - 4595
(2007/10/02)
-
- 3-Nitropropanal and 3-Nitropropanol: Preparation of the Parent Compounds and Derivatives
-
3-Nitropropanal has been prepared for the first time by 1,4-nitrite addition to acrolein.Several acetals of 3-nitropropanal are described, as well as 3-nitropropanol and some of its ethers. 3-Nitropropanol has been obtained by borane-dimethyl sulfide reduction of both 3-nitropropanal and 3-nitropropanoic acid.These reactions make available a variety of nitro compounds known as, or expected to become, highly useful and versatile building blocks for organic syntheses.
- Oehrlein, Reinhold,Schwab, Wilfried,Ehrler, Rudolf,Jaeger, Volker
-
p. 535 - 538
(2007/10/02)
-
- 2-(2-NITROETHYL)-1,3-DIOXOLANE AS REAGENT FOR 3-OXOPROPYL ANION SYNTHON: A NEW ROUTE TO JASMONOID AND PROSTAGLANDIN INTERMEDIATES
-
2-(2-Nitroethyl)-1,3-dioxolane is a versatile reagent for 3-oxopropyl anion synthon.New methodology, based on nitroaldol condensation, oxidation and direct or indirect denitration sequence is developed for the conversion of 2-(2-nitroethyl)-1,3-dioxolane into (Z)-1,4-dioxodec-7-ene, (Z)-2-(2-pentenyl)-2-cyclopenten-1-one, methyl 9,12-dioxododecanoate and methyl 7-(5-oxocyclopentenyl)heptanoate, which are popular intermediates for syntheses of (Z)-jasmonoids and prostaglandins.
- Rosini, Goffredo,Ballini, Roberto,Petrini, Marino,Sorrenti, Pietro
-
p. 3809 - 3814
(2007/10/02)
-
- α-Nitro Ketones and Esters from Acylimidazoles
-
The anion of 2-(2-nitroethyl)-1,3-dioxolane (4), prepared from the corresponding 2-bromo compound (3), undergoes condensation with acylimidazoles to give the 3-nitro-4-oxobutanal acetals (9), which can serve as valuable polyfunctional intermediates.Condensation with 1-(methoxyoxalyl)imidazole gives the tetrafunctionalized methyl 4-(1,3-dioxolan-2-yl)-3-nitro-2-oxobutanoate (13), which, however, decomposed on attempted deprotection of the ester function.The syntheses in excellent yields of simple α-nitro ketones and α-nitro esters from acylimidazoles and nitroethane and 2-nitropropane are also described.
- Crumbie, Robyn L.,Nimitz, Jonathan S.,Mosher, Harry S.
-
p. 4040 - 4045
(2007/10/02)
-