Brefeldin A derivatives and their utility in the treatment of ca

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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549270, 548525, 548256, 5482664, 5483644, 548240, 548239, 548238, 5483114, 548146, 548214, 548131, 548125, 544376, 544147, 544 2, 544 66, 544215, 540596, 540553, 540544, 514422, 514253, 5142335, 514359, 514383, 514212, 514218, 514211, 514403, 514378, 514374, 514252, 514241, 5142225, 5142292, 514397, 514365, 514372, 514364, C07D31300, C07D40512, C07D41312, A61K 31365

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056961545

ABSTRACT:
Provided are brefeldin A derivatives of the formula: ##STR1## wherein one of R.sub.1 and R.sub.2 is H and the other of R.sub.1 and R.sub.2 is a substituent group having 1 to 12 carbon atoms containing a basic nitrogen atom or a quaternary ammonium group, or a salt thereof. These derivatives exhibit good antitumor activity, and are administrable to human patients without the problems associated with brefeldin A.

REFERENCES:
Haerri, E. et al. Chemical Abstract 59, 5726h (1963).
Banerjee, P.K. et al. Design of Prodrugs, Bundgaard, H. ed. (Elsevier Science, Amsterdam), pp. 93-96 (1985).
Kovach, I.M. et al. J. Pharm. Sci. 64, 1070-1071 (1975).
Connors, T.A. Xenobiotica 16, 975-988 (1986).

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