145783-13-7Relevant articles and documents
Method for synthesizing 5-nitro-2-(propylthio) pyrimidine-4, 6-diol through continuous nitration
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Paragraph 0050-0052, (2021/06/06)
The invention discloses a method for synthesizing 5-nitro-2-(propyl thio) pyrimidine-4, 6-diol through continuous nitration. The synthesis method comprises the following steps: in a continuous flow reactor, taking nitrogen dioxide as a main nitrating agent, ozone as an auxiliary nitrating agent and 4, 6-dihydroxy-2-(propylthio) pyrimidine hydrochloride as a main raw material, carrying out nitration reaction to prepare the 5-nitro-2-(propylthio) pyrimidine-4, 6-diol compound. The method is extremely low in EHS risk, simple and convenient to operate, environment-friendly, high in production efficiency, high in yield, high in purity and suitable for industrial production.
Design, synthesis and in vitro biological evaluation of novel [1,2,3]triazolo[4,5-d]pyrimidine derivatives containing a thiosemicarbazide moiety
Geng, Peng-Fei,Liu, Xue-Qi,Zhao, Tao-Qian,Wang, Cong-Cong,Li, Zhong-Hua,Zhang, Ji,Wei, Hao-Ming,Hu, Biao,Ma, Li-Ying,Liu, Hong-Min
, p. 147 - 156 (2018/02/10)
A series of hybrid molecules containing [1,2,3]triazolo[4,5-d]pyrimidine and thiosemicarbazide moieties were designed, synthesized and evaluated for their antiproliferative activities against MGC-803, NCI-H1650 and PC-3 human cancer cells. Some of the synthesized compounds showed moderate to good activity against three selected cancer cell lines. Among these compounds, compound 29 displayed the most potent antiproliferative activity as well as good selectivity between cancer cells and normal cells. Further mechanism studies revealed that compound 29 could obviously inhibit the colony formation and migration of MGC-803 as well as induced apoptosis.
Pyrimidotriazole-containing LSD1 inhibitor, preparation method and application
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Paragraph 0054; 0055, (2017/08/31)
Belonging to the field of pharmaceutical chemistry, the invention discloses a pyrimidotriazole compound, a preparation method and application of the compound with lysine specific demethylase 1 (LSD1) as the target in preparation of antitumor drugs. The general formula of the compound is shown as I in the specification. In vitro LSD1 enzyme inhibitory activity experiments prove that by inhibiting the activity of LSD1, the compound has obvious inhibition and killing effects on multiple tumor cells, can be applied as a lead compound for further development in preparation of antitumor drugs.