Gao, Hui; Zhang, Xia; Pu, Xiao-Jia; Zheng, Xi; Liu, Bei; Rao, Gao-Xiong; Wan, Chun-Ping; Mao, Ze-Wei published the artcile< 2-Benzoylbenzofuran derivatives possessing piperazine linker as anticancer agents>, Reference of 17082-09-6, the main research area is benzofuranylcarbonylphenyl piperazinylmethylcarbonyl piperazine antitumor antiinflammatory cytotoxicity apoptosis structure activity; 2-Benzoylbenzofuran; Anticancer activity; Apoptosis; Cytotoxicity.
A series of novel 2-benzoylbenzofuran derivatives possessing a piperazine linker, I [R = H, COCH2Cl, cyclopropylsulfonyl, COC6H4CF3-4, etc.], were prepared, and their in-vitro anticancer activity against a panel of human tumor cell lines by MTT assay was evaluated. The results demonstrated that tertiary amine derivatives exhibited better cytotoxic activity, and the SAR study revealed that electron-donating substituents on the Ph ring of the derivatization functionality contributed to potent anticancer activities. Among them, compounds I [R = H, COC6H3Cl2-3,5, COCH:CHPh, CH2C6H4CH:CHCO2Me-4, CH2COMe, CH2COC6H4OMe-4] displayed both better antitumor activity and lower cytotoxic effect on human normal liver cell L02. Further apoptosis anal. showed that compound I [R = CH2C6H4CH:CHCO2Me-4] significantly induced apoptosis in A549 cell, which was considered as the most potent anticancer agent.
Bioorganic & Medicinal Chemistry Letters published new progress about Amides Role: ADV (Adverse Effect, Including Toxicity), PAC (Pharmacological Activity), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 17082-09-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C9H7ClO, Reference of 17082-09-6.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics