893-53-8Relevant academic research and scientific papers
Synthesis and bioactivity studies of 1-aryl-3-(2-hydroxyethylthio)-1-propanones
Unluer, Elif,Gul, Halise Inci,Demirtas, Alkan,Sakagami, Hiroshi,Umemura, Naoki,Tanc, Muhammet,Kazaz, Cavit,Supuran, Claudiu T.
, p. 105 - 109 (2016/12/16)
A series of Mannich bases having piperidine moiety were reacted with 2-mercaptoethanol, leading to 1-aryl-3-piperidine-4-yl-1-propanone hydrochlorides. The cytotoxicity and carbonic anhydrase inhibitory activities of these new compounds were evaluated. Among the compounds, only one derivative, nitro substituent bearing EU9, showed an effective cytotoxicity, although weak tumor specificity against human oral malignant versus nonmalignant cells. The compound induced apoptosis in HSC-2 oral squamous cell carcinoma cells, but not in human gingival fibroblast. Chemical modifications of this lead are thus necessary to further investigate it as a drug candidate and to obtain compounds with a better activity profile.
Conjugated biological molecules and their preparation
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Paragraph 0046, (2015/11/11)
Novel compounds of the general formula in which one of X and X' represents a polymer, and the other represents a hydrogen atom; each Q independently represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reductio
Dramatically accelerated synthesis of β-aminoketones via aqueous Mannich reaction under combined microwave and ultrasound irradiation
Peng, Yanqing,Dou, Ruiling,Song, Gonghua,Jiang, Jun
, p. 2245 - 2247 (2007/10/03)
An efficient green chemistry approach to the synthesis of β-aminoketones was developed under combined microwave and ultrasound irradiation. With this technique, the title compounds were rapidly synthesized in aqueous media with good yields. Georg Thieme Verlag Stuttgart.
N-substituted alpha-aminoalkylacrylophenones and some related compounds: a new class of spermicidal agents.
Gupta,Nautiyal,Jhingran,Kamboj,Setty,Anand
, p. 303 - 307 (2007/10/02)
The results of a screening program to test the spermicidal effectiveness of several compounds is presented. The program was initiated after N-substituted 3-aminoacrylophenones were found to have unexpected spermicidal activity. The compounds had been synthesized as possible antiinflammatory agents. This result prompted the synthesis and screening of N-substituted alpha-aminomethylacrylophenones, alpha-(2-aminomethyl)acrylophenones and 3-N-substituted-2-methyleneindan-1-ones. The starting materials, substituted acetophenones, for the synthesis of N-substituted alpha-aminomethylacrylophenones were either commercial products or obtained by standard methods. N-substituted amino-butyrophenone was reacted with paraformaldehyde to yield the alpha-(2 aminoethyl)acrylophenones. A series of reactions was undertaken to synthesize 2-methyleneindan-1-ones. The preparation of each is detailed and molecular formulas are provided. Spermicidal activity was assessed by dissolving the compound in physiological saline at different concentrations. 2 drops of rat sperm suspension or human semen were placed on a slide, followed by 2 drops of a compound solution. Control slides of physiological saline were prepared. The contents were mixed for approximately 5 seconds and examined under a phase contrast microscope. The results were considered positive if 100% of the spermatozoa became immotile instantaneously. Several of the compounds showed marked spermicidal activity.
