131-55-5Relevant articles and documents
Method for catalytically synthesizing ultraviolet light absorber BP-2
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Paragraph 0020; 0030-0033; 0038-0049, (2020/11/23)
The invention discloses a method for catalytically synthesizing an ultraviolet light absorber BP-2. The method comprises the following steps: (1) adding a halogenated hydrocarbon solvent and a composite catalyst into a reactor, uniform stirring and mixing, heating to 90-120 DEG C, adding 2,4-dihydroxybenzoic acid and m-diphenol into the mixture, carrying out stirring dissolving, carrying out a thermal insulation reaction for 2-3 h, after the reaction is finished, filtering while hot to recover the catalyst graphite, adding a proper amount of water into the filtrate, heating to 90-100 DEG C, completely stirring and dissolving, standing for layering, distilling an organic layer to recover a solvent, cooling a water layer to 10-20 DEG C, separating out a large amount of red crystals, carryingout suction filtration, and washing with water to obtain a crude product; and (2) dissolving the crude product with a proper amount of hot water, adding activated carbon to decolorize, boiling for 30-60 minutes, filtering while hot, cooling and crystallizing to obtain a light yellow green crystal ultraviolet light absorber BP-2 product with the melting point of 199-200 DEG C and the purity of more than or equal to 99.8%. The method is high in synthesis yield, simple in production process, high in product purity, low in cost and suitable for industrial production.
Synthesis, SAR and biological evaluation of natural and non-natural hydroxylated and prenylated xanthones as antitumor agents
Zhang, Xiaojin,Li, Xiang,Tao, Lei,Gao, Yuan,Gong, Dandan,Xi, Meiyang,Xu, Xiaoli,Guo, Qinglong,You, Qidong,Ye, Suofu,Zhang, Yu,Meng, Huyan,Zhang, Mingqian,Gao, Wenlei
, p. 1012 - 1025,14 (2012/12/12)
In order to explore the detailed structure-activity relationship (SAR) around xanthone scaffold bearing hydroxyl and prenyl moieties, twenty-nine natural and non-natural hydroxylated and prenylated xanthones have been synthesized and evaluated for their in vitro anti-proliferative activities against five human cancer cell lines, including HepG2 (hepatocelluar carcinoma), HCT-116 (colon carcinoma), A549 (lung carcinoma), BGC823 (gastric carcinoma) and MDAMB- 231 (breast carcinoma). The SAR analysis revealed that the anti-proliferative activity of the xanthones is substantially influenced by the position and number of attached hydroxyl and prenyl groups, and the presence of hydroxyl group ortho to the carbonyl function of xanthone scaffold contributes significantly to their cytotoxicity. The new prenylated xanthone 20 with a relatively simple structure, namely 1,3,8-trihydroxy-2-prenylxanthone, was found to exhibit potent antitumor activities comparable to mangostin against all the five cancer cell lines. Further mechanistic studies suggested that compound 20 induces apoptosis and causes cell cycle arrest at S phase in HepG2 cells. These results have highlighted compound 20 as a new potential lead candidate for future development of novel potent broad-spectrum antitumor agents.
Synthesis and biological evaluation of polyhydroxy benzophenone as mushroom tyrosinase inhibitors
Wu, Jianlong,Hu, Xuesen,Ma, Lin
experimental part, p. 449 - 452 (2012/01/04)
A series of polyhydroxy benzophenone were synthesized and evaluated as mushroom tyrosinase inhibitors. The results demonstrated that most of the target compounds had remarkable inhibitory activities on mushroom tyrosinase. Among all these compounds, 2,3,4,3′,4′,5′-hexahydroxy-diphenylketone 10 was found to be the most potent tyrosinase inhibitor with IC50 value of 1.4 μM. In addition, the inhibition kinetics analyzed by Lineweaver-Burk plots revealed that such compounds were competitive inhibitors. These results suggested that such compounds might be utilized for the development of new candidate for treatment of dermatological disorders.