Studies on Antitumor Cyclic Hexapeptides RA Obtained from Rubiae Radix, Rubiaceae. III. On Derivatives of RA-V and Their in Vivo Activities

概要

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With the aim of obtaining compounds with strong antitumor activity and weak toxicity, we have synthesized a series of alkylethers, fatty acid esters, benzoates and other derivatives of RA-V, an antitumor cyclic hexapeptide discovered in Rubiae Radix, and examined their antitumor activities against P-388 lymphocytic leukemia. It was found that the introduction of C_1 and C_6 chains (hydrophobic coefficient log P=about 3.2 and 5.8,respectively) on the phenol moiety of RA-V gave the most desirable compounds in terms of antitumor activity and toxicity. The caproic ester of RA-V, the n-hexylether of RA-V and RA-VII (C_1) also exhibited strong antitumor activity against other experimental tumors (L-1210 lymphocytic leukemia, B-16 melanoma and MM2 mammary carcinoma).
社団法人日本薬学会の論文
1984-08-25