K. Yasui et al., CHEMICAL MODIFICATION OF PA-48153C, A NOVEL IMMUNOSUPPRESSANT ISOLATED FROM STREPTOMYCES PRUNICOLOR PA-48153, Journal of antibiotics, 49(2), 1996, pp. 173-180
5 beta-Methoxy (20), 14-methyl (24), 14,14-dibromo-15-nor (25), 8-O-ac
yl (26 similar to 45), 8-O-alkyl (46), 8-O-alkoxycarbonyl (47, 48), an
d 8-O-carbamoyl (49) derivatives of PA-48153C, a novel immunosuppressa
nt isolated from fermentation products of Streptomyces prunicolor PA-4
8153, were prepared. These compounds were found to retain the inhibito
ry activity on the responses of both T and B cells to mitogens. Among
them, the C-8 hexanoate 28 showed potent suppressive effects on mitoge
n responses with less cytotoxicity to EL4 cells and was selected for i
n vivo evaluation.