Ten-membered ring enediynediols and enediynediones having DNA cleaving properties
AssigneeThe Scripps Research Institute
InventorsKyriacos C. Nicolaou, Erik Sorensen, Chan-Kou Hwang, Robert Discordia, Robert G. Bergman, Robert E. Minto
Life of this patent
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Abstract
Macrocyclic enediynediols and enediynediones having a ten carbon ring and open chain enediyne dihydroperoxides having eight carbons between the hydroperoxide groups that cleave DNA are disclosed, as are methods of making and using the same.
Claims8
A compound of the formula ##STR27## wherein R.sup.5 and R.sup.6 are each hydrogen or R.sup.5 and R.sup.6 together with the carbon atoms of the depicted vinylene group forms a group W that is an aromatic monocyclic ring or bicyclic fused ring system that includes five or six atoms in the ring containing the depicted vinylene group;
- and
- R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or benzyl, with the provisos that only one of R.sup.1 and R.sup.2 and one of R.sup.3 and R.sup.4 is hydrogen.
A compound of the formula ##STR28## wherein R.sup.5 and R.sup.6 are each hydrogen or R.sup.5 and R.sup.6 together with the carbon atoms of the depicted vinylene group forms a group W that is an aromatic monocyclic ring or bicyclic fused ring system that includes five or six atoms in the ring containing the depicted vinylene group;
- and
- R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or benzyl, with the provisos that only one of R.sup.1 and R.sup.2 and one of R.sup.3 and R.sup.4 is hydrogen.
Dependencies are inferred from the claim text.