title: Synthesis of pyrazole peptidomimetics and their inhibition against A549 lung cancer cells.
abstract: A series of novel pyrazole peptidomimetics was synthesized from 3-aryl-1-arylmethyl-1H-pyrazole-5-carboxylic acid and amino acid ester. Structures of the compounds were characterized by means of IR, (1)H NMR and mass spectroscopy. Compounds 5e and 5k suppress effectively the growth of A549 lung cancer cells. Preliminary research on the mechanism of action showed that the inhibition might perform through combination of apoptosis, autophagy and cell cycle arrest.
authors.affiliation: Institute of Organic Chemistry, School of Chemistry and Chemical Engineering, Shandong University, Jinan 250100, PR China.
authors.forename: Ying-Rui
authors.initials: YR
authors.lastname: Liu
authors.forename: Ji-Zhuang
authors.initials: JZ
authors.lastname: Luo
authors.forename: Pan-Pan
authors.initials: PP
authors.lastname: Duan
authors.forename: Jing
authors.initials: J
authors.lastname: Shao
authors.forename: Bao-Xiang
authors.initials: BX
authors.lastname: Zhao
authors.forename: Jun-Ying
authors.initials: JY
authors.lastname: Miao
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D017209:Apoptosis / Q000187:drug effects; D001343:Autophagy / Q000187:drug effects; D002264:Carboxylic Acids / Q000737:chemistry; D045744:Cell Line, Tumor; D059585:G1 Phase Cell Cycle Checkpoints / Q000187:drug effects; D006801:Humans; D057786:Peptidomimetics; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry* / Q000633:toxicity; D012694:Serine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D002264:Carboxylic Acids; D057786:Peptidomimetics; D011720:Pyrazoles; D012694:Serine