El-Helby, Abdel-Ghany A. published the artcileDesign, synthesis, molecular modeling, in vivo studies and anticancer activity evaluation of new phthalazine derivatives as potential DNA intercalators and topoisomerase II inhibitors, HPLC of Formula: 79-07-2, the publication is Bioorganic Chemistry (2020), 104233, database is CAplus and MEDLINE.
The design and synthesis of a new series of phthalazine derivatives I [R = -COOH, -NO2, -SO2NH2],II, III [R’ = -COOH, -NO2, -SO2NH2, -COCH3], and IV as Topo II inhibitors and DNA intercalators was designed. The synthesized compounds were in-vitro evaluated for their cytotoxic activities against HepG-2, MCF-7 and HCT-116 cell lines. Addnl., Topo II inhibitory activity and DNA intercalating affinity were investigated for the most active compounds as a potential mechanism for the anticancer activity. Compounds 3-[(3-ethyl-[1,2,4]triazolo[3,4-a]phthalazin-6-yl)amino]propan-1-ol, I [R =-SO2NH2], III [R’ = -COOH], III [R’= -NO2], and IV exhibited the highest activities against Topo II with IC50 ranging from 5.44 to 8.90μM, while compounds II and III [R’ = -COOH] were found to be the most potent DNA binders at IC50 values of 36.02 and 48.30μM, resp. Moreover, compound III [R’ = -COOH] induced apoptosis in HepG-2 cells and arrested the cell cycle at the G2/M phase. Besides, compound III [R’ = -COOH] showed Topo II poisoning effect at concentrations of 2.5 and 5μM, and Topo II catalytic inhibitory effect at a concentration of10μM. In addition, compound III [R’= -NO2] showed in-vivo a significant tumor growth inhibition effect. Furthermore, mol. docking studies were carried out against DNA-Topo II complex and DNA was investigated with the binding patterns of the designed compounds
Bioorganic Chemistry published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, HPLC of Formula: 79-07-2.
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