Yang, Kun published the artcileSynthesis, mitochondrial localization of fluorescent derivatives of cinnamamide as anticancer agents, COA of Formula: C9H10O3, the main research area is cinnamamide preparation anticancer fluorescent mitochondrial localization human; Cinnamamide; Cytotoxicity; Fluorescent image; Targeting mitochondria; Thia-Michael addition; Uptake.
The mitochondria-targeted derivatives, e.g., I were designed by the incorporation of cinnamamides into a fluorophore carrier of coumarin-3-carboxamide with a 1:1 stoichiometry. Using the amide linkers, twenty-one compounds were synthesized and the cytotoxicity against a panel of cancer cells (MCF-7, Hela, HepG2, HL-60) was tested. In particular, compound I displayed the potent cytotoxicity toward HL-60 leukemia cells, which could quickly and efficiently entry into HL-60 cells and specifically localize within mitochondria. And compound I preferred enrichment in HL-60 cells than in PBMC normal cells, accounting for the higher toxicity to cancer cells than to normal cells. Moreover, the dissipations of mitochondrial membrane potential and enhancement of cellular ROS level were also preceded upon compound I treatment, leading to cell cycle arrest and apoptosis/necrosis in HL-60 cells. Besides, acted as a Michael acceptor, compound I initiated a thia-Michael addition reaction toward cysteamine (1:2 stoichiometry), detecting by the UV-Vis spectrum and HRMS anal. This could result in the blue emission of compound I in mitochondria after the procedure of cell fixation, owing to the formation of covalent bond with mitochondrial thiols. This study reported compound I might be useful for the further development into a mitochondria-targeted anti-leukemia agent and the Michael acceptor might be a versatile functional group.
European Journal of Medicinal Chemistry published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, COA of Formula: C9H10O3.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem