123003-98-5Relevant academic research and scientific papers
Kinetic investigation of the cyclopropanation process of fullerene C60 by halogenmethyl ketones under the conditions of the Bingel reaction
Biglova, Yulya N.,Garifullin, Rustem N.,Mustafin, Akhat G.,Sakhautdinov, Ilshat M.,Sakhautdinova, Gulnaz F.
, p. 7277 - 7285 (2020/06/18)
The kinetics of the Bingel reaction with halogenmethyl ketones and C60 fullerene has been studied in streaming mode by sampling the reaction mixture at different time intervals and separating the components using HPLC. A quantum-chemical simulation of this cyclopropanation process has been carried out with the DFT method. The activation parameters of the cycloaddition process were determined theoretically and experimentally and correlated with each other. It has been revealed that the use of chloromethyl ketone as the cyclopropanation agent is preferable to its brominated analogue, and a two-fold excess of the substrate with respect to fullerene is the best option for the selective synthesis of mono-adducts.
NOVEL TRF1 MODULATORS AND ANALOGUES THEREOF
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Paragraph 0049; 0068-0069, (2020/03/26)
Novel TRF1 modulators and analogues thereof. There is provided compounds of Formula I, wherein R, R1, R2 and X have meanings written in the description. Such compounds are useful as TRF1 inhibitors and, for that reason, as medicaments, in the treatment of cancer, particularly high cancer stem cell cancer like glioblastoma and lung cancer, and can be also useful for the development of additional TRF1 inhibitors and increasing knowledge about TRF1 activity.
Phthiobuzonum derivative and its preparation and use
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Paragraph 0118; 0122, (2016/11/09)
The invention relates to a ftibamzone derivative and a preparation method and an application thereof, and belongs to the technical field of ftibamzone medicament synthesis. Pharmacological experiments prove that the ftibamzone derivative of the invention has obvious cytotoxic activity and antiviral activity, and can be used for treating viral diseases such as tumor, herpes, trachoma, and the like.
Synthesis and antiviral activity of novel 1,3,4-thiadiazine derivatives
Yang, Yajun,Feng, Ziming,Jiang, Jianshuang,Yang, Yanan,Pan, Xiandao,Zhang, Peicheng
, p. 1016 - 1019 (2011/10/08)
A series of novel 1,3,4-thiadiazine derivatives were synthesized via chemical optimization on phthiobuzone. Their anti-herpes simplex virus (HSV) activities in vitro were also tested. Several compounds exhibited more highly potent anti-HSV activity and much higher selectivity index (SI) values than those of phthiobuzone. The most potent anti-HSV compound was 4f, which showed marked inhibition against HSV-1 (IC50=77.04μg/ml) and HSV-2 (IC50=30.00μg/ml). Meanwhile it had low cytotoxicity (CC 50=1000.00μg/ml), resulting in high (SIHSV-1= 12.98, SIHSV-2=33.33, respectively). Furthermore, a computational study for prediction of absorption, distribution, metabolism, excretion (ADME) properties of compound 4f was performed by determination of topological polar surface area, absorption and Lipinski parameters.
SULFUR YLIDES. 3. SYNTHESIS OF KETO-GROUP STABILIZED AMINO-CONTAINING SULFUR YLIDES FROM AMINO ACIDS
Tolstikov, G. A.,Galin, F. Z.,Lakeev, S. N.,Khalilov, L. M.,Sultanova, V. S.
, p. 535 - 541 (2007/10/02)
An effective path of synthesis was developed of new synthetic intermediates, the optically active, keto-group stabilized amino-substituted sulfur ylides.
Synthesis of Fluorinated α-Amino Ketones, III. Preparation of Fluorinated Ketone Analogues of Phenylalanine, Lysine, and p-(Guanidino)phenylalanine
Kolb, Michael,Neises, Bernhard,Gerhart, Fritz
, p. 1 - 6 (2007/10/02)
The synthesis of α-amino mono-, di-, and trifluoromethyl and difluoromethylene ketones and their derivatives is described.A one-pot sequence related to the Dakin-West reaction starts from amino acids and gives the corresponding fluorinated ketone analogue
