Li, Shuai published the artcileDesign, synthesis and biological evaluation of erythrina derivatives bearing a 1,2,3-triazole moiety as PARP-1 inhibitors, Recommanded Product: 2-Aminobenzonitrile(Flakes or Chunks), the main research area is erythrina triazole preparation PARP 1 inhibitor antitumor structure activity; 1,2,3-Triazole; Apoptosis; Erythrina; PARP-1 inhibitor.
Inhibitors of poly (ADP-ribose) polymerase-1 (PARP-1) have shown to be promising in clin. trials against cancer, and many researchers are interested in the development of new PARP-1 inhibitors. Herein, we designed and synthesized 44 novel erythrina derivatives bearing a 1,2,3-triazole moiety, I (RR1 = O, R2 = H, 2-Me, 3-MeO, 4-Me, etc.; R = OH, R1 = H), as PARP-1 inhibitors. MTT assay results indicated that compound I (RR1 = O, R2 = 2-F) (II) had the most potent anti-proliferative activity against A549 cells among five cancer cells. The enzyme inhibitory activity in vitro of compound II was also significantly better than rucaparib. Furthermore, the selectivity index of compound II was higher than rucaparib for lung cancer cells. Flow cytometry anal. showed that compound II induced apoptosis of A549 cells by the mitochondrial pathway. Western blot anal. indicated that compound II was able to inhibit the biosynthesis of PAR effectively, and it was more potent than rucaparib. Also, compound II was able to up-regulate the ratio of bax/bcl-2, activate caspase-3, and ultimately induced apoptosis of A549 cells. The combined results revealed that the discovery of novel non-amide based PARP-1 inhibitors have great research significance and provide a better choice for the future development of drugs.
Bioorganic Chemistry published new progress about Antitumor agents. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Recommanded Product: 2-Aminobenzonitrile(Flakes or Chunks).
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts