Authors Wang, JW; Hong, G; Li, GL; Wang, WZ; Liu, TJ in MDPI published article about SIGNALING PATHWAY; NATURAL-PRODUCTS; DERIVATIVES; APOPTOSIS; DESIGN; DISCOVERY; PREDICTION; CURCUMIN; ACID in [Wang, Jiawen; Liu, Tianjun] Tianjin Univ Tradit Chinese Med, Grad Inst, Tianjin 301617, Peoples R China; [Hong, Ge; Li, Guoliang; Wang, Wenzhi; Liu, Tianjun] Chinese Acad Med Sci & Peking Union Med Coll, Inst Biomed Engn, Tianjin Key Lab Biomed Mat, Tianjin 300192, Peoples R China; [Hong, Ge; Liu, Tianjun] Chinese Acad Med Sci & Peking Union Med Coll, Inst Mat Med, State Key Lab Bioact Subst & Funct Nat Med, Beijing 100050, Peoples R China in 2019, Cited 30. Category: Pyrazines. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5
Bivalent and polyvalent inhibitors can be used as antitumor agents. In this experiment, eight ligustrazine dimers and seven ligustrazine tetramers linked by alkane diamine with different lengths of carbon chain lengths were synthesized. After screening their antiproliferation activities against five cancer cell lines, most ligustrazine derivatives showed better cytotoxicity than the ligustrazine monomer. In particular, ligustrazine dimer 8e linked with decane-1,10-diamine exhibited the highest cytotoxicity in FaDu cells with an IC50 (50% inhibiting concentration) value of 1.36 nM. Further mechanism studies suggested that 8e could induce apoptosis of FaDu cells through the depolarization of mitochondrial membrane potential and S-phase cell cycle arrest. Inspired by these results, twenty-seven additional small molecule heterocyclic dimers linked with decane-1,10-diamine and nine cinnamic acid dimers bearing ether chain were synthesized and screened. Most monocyclic and bicyclic aromatic systems showed highly selective anti-proliferation activity to FaDu cells and low toxicity to normal MCF 10A cells. The structure-activity relationship revealed that the two terminal amide bonds and the alkyl linker with a chain length of 8-12 carbon were two important factors to maintain its antitumor activity. In addition, the ADMET calculation predicted that most of the potent compounds had good oral bioavailability.
Category: Pyrazines. About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Wang, JW; Hong, G; Li, GL; Wang, WZ; Liu, TJ or concate me.
Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem