Berthel, Steven J.; Marks, Ian M.; Yin, Xuefeng; Mischke, Steven G.; Orzechowski, Lucja; Pezzoni, Gabriella; Sala, Franca; Vassilev, Lyubomir T. published the artcile< Identification of phenyl-pyridine-2-carboxylic acid derivatives as novel cell cycle inhibitors with increased selectivity for cancer cells>, Application In Synthesis of 721401-43-0, the main research area is phenylpyridine carboxylate derivative preparation structure activity antitumor cell cycle; Ro414439 cell cycle antitumor breast cancer mitosis structure activity.
Ro 41-4439, a phenyl-pyridine-2-carboxylic acid derivative, was identified by a cell-based screening approach that exploits the differences between normal and cancer cells in their sensitivity to cytotoxic agents. This compound showed low micromolar antiproliferative activity and cytotoxicity against a broad panel of human cancer cell lines in vitro, and over 10-fold selectivity to cancer cells when tested in parallel with a panel of proliferating normal human cells. Cytotoxicity of Ro 41-4439 is due to arrest of cell cycle progression in mitosis followed by induction of apoptosis. Four-week treatment of nude mice bearing established mammary tumor xenografts (MDA-MB-435) with well-tolerated doses of the compound showed 73% inhibition of tumor growth. Limited exploration of structure-activity relationships involving side chain length, and aryl and pyridine rings allowed for the identification of more potent analogs.
Anti-Cancer Drugs published new progress about Antitumor agents. 721401-43-0 belongs to class isoquinoline, and the molecular formula is C9H8BNO2, Application In Synthesis of 721401-43-0.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem