97 抗腫瘍活性環状ヘキサペプチドRA類の化学変換と構造活性相関(ポスター発表の部)

概要

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A number of antitumor cyclic hexapeptide RA derivatives, including confomation-A and B locked models, were prepared from RA-II (8), RA-V (5), RA-VII (1) and RA-X-OMc (10) for structure-activity relationship studies. Evaluation of cytotoxicity of these compounds revealed that the methoxyl group on the aryl ring of Try3 greatly influenced the activities, while the substituents on the aryl ring of Tyr6 were less important for the activities. The amide bond between D-Alal and Ser2 of RA-III (25) was selectively cleaved via an oxazoline intermediate (28) to afford the seco-RA-III derivative (31). Inactiveness of the seco derivative against tumor cells revealed the importance of 18 membered ring structure, however the observations that the various ring modified derivatives including confomationally locked model compounds showed singnificant cytotoxicities suggested that further study was required for elucidating the biologically active confomation of RAs.
天然有機化合物討論会の論文
1992-09-10