Oekchuae, Sittisak published the artcileThe Design and Synthesis of a New Series of 1,2,3-Triazole-Cored Structures Tethering Aryl Urea and Their Highly Selective Cytotoxicity toward HepG2, Recommanded Product: 2-Aminobenzonitrile(Flakes or Chunks), the main research area is triazole cored aryl urea preparation antitumor human; 1,2,3-triazole-containing drug; click reaction; drug discovery; hepatocellular carcinoma (HCC); selective anti-HepG2 agent; sorafenib analog; targeted cancer drug.
Herein, a new series of 1,2,3-triazole-cored structures incorporating aryl urea I [R = H, 2-Me, 4-F, etc.] as anti-HepG2 agents was designed and synthesized via nucleophilic addition and copper-catalyzed azide-alkyne cycloaddition (CuAAC) with excellent yields. Significantly, almost all triazole-cored analogs exhibited less cytotoxicity toward normal cells, human embryonal lung fibroblast cell MRC-5, compared to Sorafenib and Doxorubicin. Among them, I [R = 2-OEt, 2-Cl] exhibited the highest selectivity indexes (SI = 14.7 and 12.2), which were ca. 4.4- and 3.7-fold superior to that of Sorafenib (SI = 3.30) and ca. 3.8- and 3.2-fold superior to that of Doxorubicin (SI = 3.83), resp. Addnl., excellent inhibitory activity against hepatocellular carcinoma HepG2, comparable to Sorafenib, was still maintained. A cell-cycle anal. and apoptosis induction study suggested that I [R = 2-OEt, 2-Cl] likely share a similar mechanism of action to Sorafenib. Furthermore, compounds I [R = 2-OEt, 2-Cl] exhibit appropriate drug-likeness, analyzed by SwissADME. With their excellent anti-HepG2 activity, improved selectivity indexes, and appropriate druggability, the triazole-cored analogs I [R = 2-OEt, 2-Cl] are suggested to be promising candidates for development as targeted cancer agents and drugs used in combination therapy for the treatment of HCC.
Pharmaceuticals 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