title: Cytotoxicity of aporphines in human colon cancer cell lines HCT-116 and Caco-2: an SAR study.
abstract: A series of synthetic aporphine derivatives structurally related to domesticine and nantenine (ring A, N6 and ring C truncated analogs), was evaluated in MTS cytotoxicity assays against the human colon cancer cell lines, HCT-116 and Caco-2. In general, the C1 position of ring A is tolerant of alkoxy substituents as well as a benzoyl ester functionality. Other modifications evaluated resulted in a decrease in cytotoxic activity. The most potent compounds identified had IC(50) values in the range 23-38 μM, comparable to the known cytotoxic agent, etoposide.
authors: Chemistry Department, Hunter College, CUNY, New York, NY 10065, USA.
authors: Shashikanth
authors: S
authors: Ponnala
authors: Sandeep
authors: S
authors: Chaudhary
authors: Antonio
authors: A
authors: González-Sarrias
authors: Navindra P
authors: NP
authors: Seeram
authors: Wayne W
authors: WW
authors: Harding
mesh_terms: D001060:Aporphines / Q000737:chemistry* / Q000627:therapeutic use / Q000633:toxicity; D018938:Caco-2 Cells; D003110:Colonic Neoplasms / Q000188:drug therapy; D004354:Drug Screening Assays, Antitumor; D045325:HCT116 Cells; D006801:Humans; D013329:Structure-Activity Relationship
chemical_list: D001060:Aporphines; C454302:domesticine; C041615:nantenine