title: Novel small molecules as apoptosis inducers: synthesis, preliminary structure-activity relationships, and in vitro biological evaluation.
abstract: Inducing apoptosis is a promising therapeutic approach to overcome cancer. In this study, 30 compounds were synthesized and evaluated for their antiproliferative activity against three tumor cell lines in vitro: A875, H460 and Hela cancer cells by the MTT assay. The most potent analogue 7a, a novel compound was first reported by our group, inhibited the proliferation of A875 cells with an IC50 value of 98 nM. Flow cytometry analysis and morphological analysis suggested that compound 7a had potential anticancer efficacy via G2/M cell cycle arrest, which could be attributed to its proliferation and apoptosis, and also in a concentration-dependent manner. The SAR analysis indicated that the substituents R(2) played a crucial role in the antiproliferation activity.
authors.affiliation: State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, Sichuan, China.
authors.forename: Lifeng
authors.initials: L
authors.lastname: Zhao
authors.forename: Xiao
authors.initials: X
authors.lastname: Li
authors.forename: Lidan
authors.initials: L
authors.lastname: Zhang
authors.forename: Tinghong
authors.initials: T
authors.lastname: Ye
authors.forename: Yongxia
authors.initials: Y
authors.lastname: Zhu
authors.forename: Yuquan
authors.initials: Y
authors.lastname: Wei
authors.forename: Shengyong
authors.initials: S
authors.lastname: Yang
authors.forename: Luoting
authors.initials: L
authors.lastname: Yu
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D048708:Cell Growth Processes / Q000187:drug effects; D045744:Cell Line, Tumor; D002722:Chlorobenzenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000577:Amides; D000970:Antineoplastic Agents; D002722:Chlorobenzenes; D011725:Pyridines; D013830:Thiadiazoles