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 0008; 0045-0050; 0053-0064, (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.
Pyrimidine and triazole containing LSD1 inhibitor and preparation method and application thereof
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Paragraph 0082; 0083, (2017/04/03)
The invention belongs to the field of medicinal chemistry, and discloses a pyrimidine and triazole containing compound and a preparation method and application thereof in preparation of anti-cancer medicine with lysine specific demethylase 1 (LSD1) being a target. The general formula of the compound is shown in the drawing I. In-vitro LSD1 enzyme inhibition activity experiments prove that by inhibiting LSD1 activity, the compound has obvious inhibiting and killing effects on kinds of cancer cells and can be applied to preparation of the anti-cancer medicine as a further developed lead compound.