European Journal of Organic Chemistry · 2008 · 30 citations · 17 references
PharmacyMedicinal ChemistryPharmacologyBiochemical PharmacologyCancer PharmacologyDrug DiscoveryPeptide ChemistryPeptide Drug DiscoveryAnticancer ActivityAnticancer Natural ProductsAntiprotozoal ChemotherapyAntiprotozoal PharmacologyClonogenic Survival AssaysPeptide Medicinal Chemistry
Abstract The cyclic dodecapeptides tychonamide A ( 1 ) and B ( 2 ) isolated from the methanolic extract of the cyanobacterium Tychonema sp. contain the novel β‐amino acid 3‐amino‐2,5,7‐trihydroxy‐8‐phenyloctanoic acid (Atpoa). Compounds 1 and 2 have cytotoxic activity towards cancer cell linesin a monolayer assay with mean IC 50 values of 0.9 and 3.3 μg mL –1 , respectively. Compound 2 was shown to be active against tumor cell suspensions derived fromsolid tumor xenografts in a clonogenic assay (mean IC 50 2.4 μg mL –1 ). Additionally, antiprotozoal activity was observed ( Trypanosoma b. rhodesiense , IC 50 0.1 μg mL –1 ) for compound 1 . (© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2008)
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