ABSTRACT
Most of the 10-substituted triazolylartemisinin synthesized via the Huisgen 1,3-dipolar cylcoaddition of diastereomeric 10-azidoartemisinin (5, 6, and 7) with various alkynes (a-h) exhibit strong growth inhibition activity, even at sub-micromolar concentrations, against various cancer cell lines such as DLD-1, U-87, Hela, SiHa, A172, and B16. In particular, 10b and 10f showed a highly strong cytotoxicity.
Subject(s)
Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Artemisinins/chemical synthesis , Artemisinins/pharmacology , Antineoplastic Agents/chemistry , Artemisinins/chemistry , Cell Line, Tumor , Cyclization , Humans , Magnetic Resonance SpectroscopyABSTRACT
Sargahydroquinoic acid (2), a major active constituent of Sargassum micracanthum collected from the coast of the East Sea in Korea, showed a selective vasodilatation effect on the basilar arteries of rabbits. Therefore, treatment with sargahydroquinoic acid may selectively accelerate cerebral blood flow through dilatation of the basilar artery without lowering systemic blood pressure.
Subject(s)
Alkenes/chemistry , Alkenes/pharmacology , Basilar Artery/drug effects , Benzoquinones/chemistry , Benzoquinones/pharmacology , Animals , Molecular Structure , Rabbits , Sargassum/chemistry , Vasodilation/drug effectsABSTRACT
In order to discover novel multidrug resistance (MDR) reversal agents for efficient cancer chemotherapy, the unsymmetrical curcumin mimics with various amide moieties (6-19) were synthesized and evaluated their MDR reversal activities in MDR cell line KBV20C. Among the tested compounds, 13, 16, and 17 showed potent MDR reversal activities by inhibiting drug efflux function of P-glycoprotein in KB20C cells, and almost recovered the cytotoxicity of vincristine and paclitaxel against KBV20C cell to the degree of potency against drug sensitive KB cells.
