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Paper | Regular issue | Vol 36, No. 8, 1993, pp.1837-1843
Published online, 1st January, 1970
DOI: 10.3987/COM-93-6382
Preparation of [Cys2]-RA-VII; The First Sulfur Containing Analogue of RAS Possessing Antitumor Activity

Hideji Itokawa,* Kazuyuki Kondo, Yukio Hitotsuyanagi, and Koichi Takeya

*Department of Pharmacognosy, Tokyo College of Pharmacy , 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan


RA-III (2), a potent antitumor cyclic hexapeptide, has been converted to [Cys2]-RA-VII (5) via thiolacetate (3). Derivatives (3) and (5) showed antitumor activities against P388 leukemia cells in vitro and in vivo.