Abstract: This invention provides aryl-substituted acyclic enediyne compounds of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1=R2=H; or R1 and R2 together form a moiety represented by the formula R3 represents a substituted or unsubstituted alkyl having 4-30 carbon atoms, or a substituted or unsubstituted aryl group having 3-30 carbon atoms; and R4 represents a substituted or unsubstituted aryl group having 3-30 carbon atoms; with the proviso that R3 is not butyl, pentyl, tetrahydropyranyloxymethyl, tetrahydropyranyloxypropyl or phenyl when R1=R2=H and R4 is o-cyanophenyl,; and with the proviso that R3 is not butyl when R1=R2=H and R4 is phenyl. The compounds of formula (I) are found to have inhibitory activities against topoisomerase I or act as a S phase or G2/M phase blocker.

Abstract: This invention provides aryl-substituted acyclic enediyne compounds of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1?R2?H; or R1 and R2 together form a moiety represented by the formula ?R3 represents a substituted or unsubstituted alkyl having 4-30 carbon atoms, or a substituted or unsubstituted aryl group having 3-30 carbon atoms; and ?R represents a substituted or unsubstituted aryl group having 3-30 carbon atoms; with the proviso that R3 is not butyl, pentyl, tetrahydropyranyloxymethyl, tetrahydropyranyloxypropyl or phenyl when R1?R2?H and R4 is o-cyanophenyl,; and with the proviso that R3 is not butyl when R1?R2?H and R4 is phenyl. The compounds of formula (I) are found to have inhibitory activities against topoisomerase I or act as a S phase or G2/M phase blocker.

Abstract: A pharmaceutical compositions comprises a compound of formula (I): or a pharmaceutically acceptable salt thereof: wherein R1?R2 ?H; or R1 and R2 together form a moiety represented by the formula R3 represents a substituted or unsubstituted alkyl having 4-30 carbon atoms, or a substituted or unsubstituted aryl group having 3-30 carbon atoms; and R4 represents a substituted or unsubstituted aryl group having 3-30 carbon atoms; with the proviso that R3 is not butyl, pentyl, tetrahydropyranyloxymethyl, tetrahydropyranyloxypropyl or phenyl when R1?R2?H and R4 is o-cyanophenyl,; and with the proviso that R3 is not butyl when R1?R2?H and R4 is phenyl. The pharmaceutical composition may be used to treat a subject afflicted with a tumor/cancer by inhibiting topoisomerase I activities or blocking the S phase or G2/M phase of the tumor/cancer cells.