Preparation and cytotoxicity of cyclic hexapeptides, RA derivatives

Article abstract of DOI:10.1248/cpb.41.1266

Several aromatic ring substituent modified RA derivatives were prepared from RA-VII (I), RA-V (8) and RA-II (II), and evaluated for cytotoxicity against P388 leukemia and KB cells. In terms of IC₅₀ values, the C(ζ) methoxyl group of Tyr-3 greatly influenced the activities, while the substituents at the C(ζ) position of Tyr-6 were less important. One of the derivatives, Tyr-6-C(ζ)-deoxyRA-V (9, P388, IC₅₀, 0.0025μg/ml) was nearly as active as RA-VII (1, 0.0013 μg/ml), and also expressed promising anti- P388 in vivo activity (test/control = 171%, at 25 mg/kg).

Full text of DOI:10.1248/cpb.41.1266

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