6632-68-4Relevant articles and documents
-
Abramova et al.
, (1978)
-
5,6-amino -1,3-dihydrocarbyl substituted uracil and preparation method thereof (by machine translation)
-
Paragraph 0044-0046, (2020/05/09)
The invention belongs to the technical field of fine chemical engineering, and particularly relates to 5,6 -amino - 1111,dihydrocarbyl substituted uracil and a preparation method, of the dihydrocarbyl-substituted uracil 5,6 - diamino - 1111, 3-dihydrocarbyl- R substituted uracil, 5,6 - as shown in Formula (I). 1 And R2 Hydrochloride gas 1 - 10, each independently selected from hydrogen or carbon chain lengths of, carbon atoms according to the present invention 5,6 - of the present invention PVC diamino - 1111, 3-dihydrocarbyl-substituted uracil capable of absorbing, degradation processes, can also produce synergistic effect PVC by substituting labile chlorine atoms, with zinc stearate and calcium stearate PVC in combination with zinc stearate and calcium stearate for PVC to have better stabilization effect, The process performance, is improved PVC DEG, with good, stabilization effect PVC in combination. Heat stability 5,6 - can also be produced by the method, of the PVC present invention, for PVC, % of the stable effect of the present invention. (by machine translation)
Synthesis method of theophylline
-
Paragraph 0046-0048, (2020/12/29)
The invention discloses a synthesis method of theophylline, and relates to the technical field of preparation of heterocyclic compounds containing purine ring systems. The preparation method comprisesthe following steps: mixing cyanoacetic acid and acetic anhydride at 30-80 DEG C for reaction, adding a solvent and dimethylurea, cooling to room temperature after reflux reaction is finished, filtering, concentrating filtrate, combining solids to obtain dimethylacetamide, adding liquid caustic soda to adjust the pH to 8-11, and reacting at 80-100 DEG C to generate dimethyl 4AU; completely dissolving dimethyl 4AU in formic acid, adding sodium nitrite, reacting at room temperature, adding a catalyst and water, keeping the temperature at 30-70 DEG C, recovering the catalyst after the reaction is finished, and concentrating mother liquor to recover formic acid, thereby obtaining dimethyl FAU; adding dilute sulfuric acid into the dimethyl FAU to adjust the pH value to 36, heating to 90-100 DEG C, allowing the feed liquid to pass through an ozone reactor and a decolorizer, crystallizing by a crystallizer, and carrying out cold filtration to obtain theophylline. The method has the advantages of few reaction steps, mild reaction conditions, simple operation, high yield, stable product quality, small discharge capacity, reduction of the environmental protection treatment difficulty, and easy industrialization.
EGFR inhibitors and apoptotic inducers: Design, synthesis, anticancer activity and docking studies of novel xanthine derivatives carrying chalcone moiety as hybrid molecules
Abou-Zied, Hesham A.,Youssif, Bahaa G.M.,Mohamed, Mamdouh F.A.,Hayallah, Alaa M.,Abdel-Aziz, Mohamed
, (2019/05/29)
One of the helpful ways to improve the effectiveness of anticancer agents and weaken drug resistance is to use hybrid molecules. therefore, the current study intended to introduce 20 novel xanthine/chalcone hybrids 9–28 of promising anticancer activity. Compounds 10, 11, 13, 14, 16, 20 and 23 exhibited potent inhibition of cancer cells growth with IC50 ranging from 1.0 ± 0.1 to 3.5 ± 0.4 μM compared to doxorubicin with IC50 ranging from 0.90 ± 0.62 to 1.41 ± 0.58 μM and that compounds 11 and 16 were the best. To verify the mechanism of their anticancer activity, compounds 10, 11, 13, 14, 16, 20 and 23 were evaluated for their EGFR inhibitory effect. The study results revealed that compound 11 showed IC50 = 0.3 μM on the target enzyme which is more potent than staurosporine reference drug (IC50 = 0.4 μM). Accordingly, the apoptotic effect of the most potent compounds 11 was extensively investigated and showed a marked increase in Bax level up to 29 folds, and down-regulation in Bcl2 to 0.28 fold, in comparison to the control. Furthermore, the effect of compound 11 on Caspases 3 and 8 was evaluated and was found to increase their levels by 8 and 14 folds, respectively. Also, the effect of compound 11 on the cell cycle and its cytotoxic effect were examined. Moreover, a molecular docking study was adopted to confirm mechanism of action.
