4779-37-7Relevant academic research and scientific papers
Microwaves assisted synthesis of antitumor agents of novel azoles, azines, and azoloazines pendant to phenyl sulfone moiety and molecular docking for VEGFR-2 kinase
Abdulwahab, Hanan Gaber,Alsaedi, Amani M. R.,Farghaly, Thoraya A.,Shaaban, Mohamed R.
, (2021/10/21)
The present research article contains two valuable starting phenylsulfone-enaminones which were synthesized in short reaction time with excellent yield under microwaves irradiation. These two enaminones were reacted with both nucleophiles and electrophiles to afford novel heterocycles bearing phenylsulfone moiety. The structure of all prepared phenylsulfone derivatives as well as their mechanistic pathways were studied based on their spectral data. Moreover, seventeen phenylsulfone derivatives were screened in vitro for their anticancer activity against HepG-2 and HCT-116 cell lines. Compounds 4 and 7a were equipotent to doxorubicin against HepG-2 cell line. Moreover, diphenyl sulfone derivative 7a was 3-fold more potent than doxorubicin against human colon cancer cell line with IC50 = 3.13 and 9.4 μg/mL, respectively. Remarkably, compound 7b was 2-fold more active than doxorubicin against the two tested cell lines. A docking study of title compounds into VEGFR-2 kinase was also conducted.
Synthesis and antimicrobial evaluation of novel pyrazolopyrimidines incorporated with mono- And diphenylsulfonyl groups
Alsaedi, Amani M.R.,Farghaly, Thoraya A.,Shaaban, Mohamed R.
, (2019/11/19)
A novel series of pyrazolo[1,5-a]pyrimidine ring systems containing phenylsulfonyl moiety have been synthesized via the reaction of 2-(phenylsulfonyl)-1-(4-(phenylsulfonyl) phenyl)ethan-1-one, 2-benzenesulfonyl-1-(4-benzenesulfonyl-phenyl)-3-dimethylamino-propenone and 3-(dimethylamino)-1-(4-(phenylsulfonyl)phenyl)prop-2-en-1-one each with various substituted aminoazopyrazole derivatives in one pot reaction strategy. The proposed structure as well as the mechanism of their reactions were discussed and proved with all possible spectral data. The results of antimicrobial activities of the new sulfone derivatives revealed that several derivatives showed activity exceeding the activity of reference drug. Contrary to expectations, we found that derivatives containing one sulfone group are more effective against all bacteria and fungi used than those contain two sulfone groups.
Catalytic dehydrogenative dual functionalization of ethers: Dealkylation-oxidation-bromination accompanied by C-O bond cleavage: Via aerobic oxidation of bromide
Moriyama, Katsuhiko,Hamada, Tsukasa,Nakamura, Yu,Togo, Hideo
supporting information, p. 6565 - 6568 (2017/07/10)
Catalytic dehydrogenative dual functionalization (DDF) of ethers via oxidation, dealkylation, and α-bromination by the aerobic oxidation of bromide was developed to obtain the corresponding α-bromo ketones in high yields. In particular, the reaction of substituted tetrahydrofurans as cyclic ethers provided 3,3-dibromo tetrahydrofuran-2-ols in high yields selectively through the double α-bromination.
BIARYL INHIBITORS OF THE SODIUM CHANNEL
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Page/Page column 54; 55, (2013/09/12)
The invention relates to compounds useful in treating conditions associated with voltage- gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns biaryl derivatives (e.g., compounds according to any of Formulas (I)-(XII) or Compounds (l)-(372) of Table 1) that are that are useful in treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's Disease, mood disorders, schizophrenia, psychosis, tinnitus, amyotropic lateral sclerosis, glaucoma, ischaemia, spasticity disorders, obsessive compulsive disorder, restless leg syndrome and Tourette syndrome.
Synthesis and evaluation of non-dimeric HCV NS5A inhibitors
Amblard, Franck,Zhang, Hongwang,Zhou, Longhu,Shi, Junxing,Bobeck, Drew R.,Nettles, James H.,Chavre, Satish,McBrayer, Tamara R.,Tharnish, Philip,Whitaker, Tony,Coats, Steven J.,Schinazi, Raymond F.
, p. 2031 - 2034 (2013/05/09)
Based on the symmetrical bidentate structure of the NS5A inhibitor BMS-790052, a series of new monodentate molecules were designed. The synthesis of 36 new non-dimeric NS5A inhibitors is reported along with their ability to block HCV replication in an HCV 1b replicon system. Among them compound 5a showed picomolar range activity along with an excellent selectivity index (SI > 90,000).
