119730-08-4Relevant academic research and scientific papers
Novel Aryl-Substituted Pyrimidones as Inhibitors of 3-Mercaptopyruvate Sulfurtransferase with Antiproliferative Efficacy in Colon Cancer
Bantzi, Marina,Augsburger, Fiona,Loup, Jérémie,Berset, Yan,Vasilakaki, Sofia,Myrianthopoulos, Vassilios,Mikros, Emmanuel,Szabo, Csaba,Bochet, Christian G.
, p. 6221 - 6240 (2021/05/06)
The enzyme 3-mercaptopyruvate sulfurtransferase (3-MST) is one of the more recently identified mammalian sources of H2S. A recent study identified several novel 3-MST inhibitors with micromolar potency. Among those, (2-[(4-hydroxy-6-methylpyrimidin-2-yl)sulfanyl]-1-(naphthalen-1-yl)ethan-1-one) or HMPSNE was found to be the most potent and selective. We now took the central core of this compound and modified the pyrimidone and the arylketone sides independently. A 63-compound library was synthesized; compounds were tested for H2S generation from recombinant 3-MST in vitro. Active compounds were subsequently tested to elucidate their potency and selectivity. Computer modeling studies have delineated some of the key structural features necessary for binding to the 3-MST's active site. Six novel 3-MST inhibitors were tested in cell-based assays: they exerted inhibitory effects in murine MC38 and CT26 colon cancer cell proliferation; the antiproliferative effect of the compound with the highest potency and best cell-based activity (1b) was also confirmed on the growth of MC38 tumors in mice.
5 H - thiazolo [3, 2 - a] pyrimidine - 5 - ketone derivative and its preparation method and used as antibacterial medicament application
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Paragraph 0039; 0086-0088, (2017/08/23)
The invention discloses 5H-thiazolo[3,2-a]pyrimidyl-5-one derivatives which have a definite chemical structure and are simple in chemical structure. The invention also discloses a preparation method of the 5H-thiazolo[3,2-a]pyrimidyl-5-one derivatives, wh
Synthesis of some new thiazolo[3,2-A]pyrimidine derivatives and screening of their in vitro antibacterial and antitubercular activities
Cai, Dong,Zhang, Zhi-Hua,Chen, Yu,Yan, Xin-Jia,Zhang, Shi-Ti,Zou, Liang-Jing,Meng, Li-Hong,Li, Fang,Fu, Bing-Jie
, p. 292 - 302 (2016/01/25)
The novel 5H-thiazolo[3,2-A]pyrimidin-5-ones were synthesized by thiophene ring closure. The first step is the synthesis of S-alkylated derivatives by the reaction of 6-substituted-2-thiouracils with the appropriate substituted phenacyl halides. Upon trea
The Chemistry of Pyrimidinethiols. II. The Preparation and Reaction of Some 2-Arenecarbonylmethylthiopyrimidines
Hurst, Derek T.,Beaumont, Claire,Jones, Derek T. E.,Kingsley, Deborah A.,Partridge, Julian D.,Rutherford, Trevor J.
, p. 1209 - 1219 (2007/10/02)
A number of 2-arenecarbonylmethylthiopyrimidin-4(1H)-ones has been synthesized.Those having H, Me or Pr as a 6-substituent undergo ready sulfur extrusion on heating in diphenyl ether to give 2-(arenecarbonylmethylene)-2,3-dihydropyrimidin-4(1H)-ones, but
