A number of [N-alky-Al@A-VII derivatives have been prepared from RA-VII (1) and evaluated for in vitro antitumor activity against P388 and KB cells, and partly for in vivo anti-P388 activity. All analogues retained significant cytotoxicity, and N-prenyl derivative (2j) showed more promising in vivo activity than 1. RAs, antitumor cyclic hexapeptides, have been isolated from Japanese and Chinese medicinal plants of the genuses Rubic ukune and R cordifilia (Rubiaceae), and particular interest has centered on the unique bicyclic structure and antitumor activity of them? RA-VII (l), the most potent congener of RAs is now under clinical trial in Japan as an anticancer agent. 3 1 is potentially promising anticancer agent, but its rather high toxicity restricted the doses and schedule for administration.3 To find a lower toxic alternative, we have undertaken chemical modification of 1. Derivation of 1 has been difficult thus far due to the lack of a suitable functional structure, and only 0-acylation or O-alkylation of the phenolic hydroxyl group of RA-V (Ty#de-&nethylRA-VII) has been extensively studied.4 Another possible part for modifications seemed to be the amide nitrogen of Ak?, at which a methyl group could be introduced by excess amount of methyl iodide and KF-alumina? Recently we found that under the phase transfer conditions the amide nitrogen is effectively alkylated withN, Ndialkylaminoethyl chloride without any racemixation of the constituting amino acid residues6 By using various alkylating agent, this method is found to be applicable to prepare the corresponding N-alkylated dexhtives. In this report we will describe the preparation and biological evaluation of a number of ~-all+Ala2m-VU derivatives.