Shang, Hai; Li, Lingyu; Ma, Liyan; Tian, Yu; Jia, Hongmei; Zhang, Tao; Yu, Meng; Zou, Zhongmei published the artcile< Design and synthesis of molecular hybrids of sophora alkaloids and cinnamic acids as potential antitumor agents>, Category: naphthyridine, the main research area is sophora alkaloid cinnamic acid hybrid preparation SAR antitumor apoptosis; antitumor; apoptosis; cinnamic acid; hybrid; sophora alkaloid.
Twenty-five sophora alkaloids-cinnamic acid hybrids, including matrine-cinnamic acid hybrids I (R1 = H, Cl; R2 = H, OMe, Cl, Br; R3 = H, CF3, NO2, etc.; R4 = H, OMe; -R2R3- = -OCH2O-), sophoridine-cinnamic acid hybrids II (R1 = H, Cl; R2 = H, Cl, Br; R3 = H, OMe, NO2, etc.; R4 = H; -R2R3- = -OCH2O-), and sophocarpine-cinnamic acid hybrids III (R1 = H, Cl; R2 = R4 = H; R3 = H, OMe), were designed, synthesized, and evaluated in vitro against three human tumor cell lines (HeLa, HepG2 and A549) with cisplatin as a pos. control. Some matrine-cinnamic acid and sophoridine-cinnamic acid compounds exhibited potent effect against all three cancer cell lines, such as compounds I (R1 = Cl; R2 = R3 = R4 = H), I (R1= R4 = H; R2 = R3 = Cl), I (R1 = R2 =R4= H; R3 = CF3) and I (R1 = R2 = R4 = H; R3 = Cl). The structure-activity relationship study of the synthesized compounds was also performed. Preliminary mechanistic studies indicated that compounds I (R1= R4 = H; R2 = R3 = Cl) and I (R1 = R2 = R4 = H; R3 = Cl) could induce apoptosis in HepG2 cell line. Further, compounds I (R1= R4 = H; R2 = R3 = Cl) and I (R1 = R2 = R4 = H; R3 = Cl) altered mitochondrial membrane potential and produced ROS leading to cell apoptosis of HepG2 cells. Overall, findings suggested that these compounds may provide promising lead compounds for further development as antitumor agents by structural modification.
Molecules published new progress about Alkaloids Role: PAC (Pharmacological Activity), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Category: naphthyridine.
Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem