Discovery of indoline derivatives that inhibit esophageal squamous cell carcinoma growth by Noxa mediated apoptosis.
A series of novel indoline derivatives were synthesized and evaluated for antiproliferative activity against four selected cancer cell lines (Hela, A549, HepG2 and KYSE30). Among them, compound 20 displayed the potent inhibition activity against esophageal cancer cells (Kyse30, Kyse450, Kyse510 and EC109). Cellular mechanism studies in esophageal squamous cell carcinoma (ESCC) cells elucidated compound 20 inhibited cell growths in vitro and in vivo, reduced colony formation, arrested cell cycle at M phase, and induced Noxa-dependent apoptosis in ESCC. Importantly, compound 20 was identified as a novel Noxa mediated apoptosis inducer. These results suggested that compound 20 might be a promising anticancer agent with potential for development of further clinical applications.
['Fu|Dong-Jun|DJ|', 'Li|Miaomiao|M|', 'Zhang|Sai-Yang|SY|', 'Li|Jiang-Feng|JF|', 'Sha|Beibei|B|', 'Wang|Longhao|L|', 'Zhang|Yan-Bing|YB|', 'Chen|Ping|P|', 'Hu|Tao|T|']
D000970:Antineoplastic Agents D017209:Apoptosis D059447:Cell Cycle Checkpoints D045744:Cell Line, Tumor D049109:Cell Proliferation D004354:Drug Screening Assays, Antitumor D004938:Esophageal Neoplasms D000077277:Esophageal Squamous Cell Carcinoma D006801:Humans D007211:Indoles D015394:Molecular Structure D019253:Proto-Oncogene Proteins c-bcl-2 D034741:RNA, Small Interfering D013329:Structure-Activity Relationship
Indoline Esophageal squamous cell carcinoma Cell growths in vitro and in vivo Noxa-dependent apoptosis