CC-1065 analogs

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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548421, 435119, 435169, C07D48704, C07D48708, A61K 3140

Patent

active

053328370

ABSTRACT:
This invention concerns 2-acyl-4,5,8,8a-tetrahydro-4-oxycyclopropan[c]pyrrol(3,2-e) indole derivatives of Formula I': ##STR1## the compounds of Formula I' are useful as uv light absorber substances, as chemical intermediates and as prodrugs of known spirocyclopropylpyrroloindole CC-1065 analogs. Representative Formula I' compounds have been shown to possess useful ranges of antitumor activity in standard laboratory animal tests.

REFERENCES:
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Burger, A. "A guide to the chemical basis of drug design" John Wiley & Sons, N.Y. 1984 p. 15.
Korolkovas, A. Essentials of Medicinal Chemistry. 2nd ed. (1988). John Wiley & Sons:New York. pp. 102-103.
Bundgaard, H. (Ed.). Design of Prodrugs. (1985). Elsevier:Amsterdam. pp. 1-9.
Sinkula, A. A. and S. H. Yalkowsky. "Rationale for Design of Biologically Reversible Drug Derivatives: Prodrugs," Journal of Pharmaceutical Sciences, 64:2 (Feb. 1975), 181-210.
Sinkula, A. A. "Prodrug Approach in Drug Design," Ann. Rep. Med. Chem., 10 (1975), 306-316.

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