Li, Shuai published the artcileDesign, synthesis and biological evaluation of homoerythrina alkaloid derivatives bearing a triazole moiety as PARP-1 inhibitors and as potential antitumor drugs, HPLC of Formula: 1885-29-6, the main research area is homoerythrina alkaloid triazole preparation antitumor PARP 1 inhibitor; 1,2,3-Triazole; Antitumor; Apoptosis; Drug discovery; Homoerythrina alkaloid; PARP-1 inhibitor.
A series of homoerythrina alkaloid derivatives containing a 1,2,3-triazole moiety as PARP-1 inhibitors were designed and synthesized. And their anti-proliferative activity was further evaluated. Compound I had excellent activity to inhibit proliferation of A549 cells (IC50 = 1.89μM), which was higher than harringtonine (IC50 = 10.55μM), pemetrexed (IC50 = 3.39μM), and rucaparib (IC50 = 4.91μM). Furthermore, the selectivity index of compound I was higher than rucaparib and pemetrexed for lung cancer cells. Flow cytometry anal. showed that compound I significantly arrested the cell cycle in the S phase, then induced apoptosis of A549 cells (apoptosis rate is 46%), which effectively inhibited cell proliferation. Simultaneously, western blot anal. revealed that compound I could prevent the biosynthesis of PAR. Further anal. results revealed that compound I could inhibit the expression of cyclin A, down-regulate the expression of bcl-2/bax, activate caspase-3, and ultimately induce apoptosis of A549 cells. All the results indicated that compound I had potential research value as a novel PARP-1 inhibitor in antitumor, and it provided a new reference for further development of PARP-1 inhibitors.
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, HPLC of Formula: 1885-29-6.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts