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; andR4 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.
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机译：本发明提供式（I）的芳基取代的无环二烯化合物： 或其药学上可接受的盐或溶剂化物，其中 R 1 = R 2 = H;或R 1 和R 2 一起形成由式 ; R 3 表示具有4-30个碳原子的取代或未取代的烷基，或具有3-30个碳原子的取代或未取代的芳基;和 R 4 表示具有3-30个碳原子的取代或未取代的芳基; ，条件是当R 1 =时，R 3 不是丁基，戊基，四氢吡喃氧基甲基，四氢吡喃氧基丙基或苯基。 R 2 = H，R 4 为邻氰基苯基;并且当R 1 = R 2 = H和R 4 为R时，R 3 不是丁基苯基。 ;发现式（I）化合物具有对拓扑异构酶I的抑制活性或充当S期或G2 / M期阻滞剂。
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