(e)-styryl sulfone anticancer agents

Details (e)-styryl sulfone anticancer agents (e)-styryl sulfone anticancer agents

C - Chemistry, Metallurgy

07

C

C07C 317/10 (2006.01) A61K 31/10 (2006.01) A61K 31/277 (2006.01) A61P 35/00 (2006.01) C07C 315/04 (2006.01) C07C 317/18 (2006.01) C07C 317/28 (2006.01) C07C 317/44 (2006.01)

Patent

CA 2366750

(E)-styryl benzylsulfones of formula (I) are useful as anticancer agents wherein R1, R2, R3, and R4 are independently selected from the group consisting of hydrogen, fluoro, chloro, iodo, bromo, C1-C6 alkyl, C1-C4 alkoxy, nitro, cyano and trifluoromethyl, with the proviso that (a) R1, R2, and R3 not all hydrogen when R4 is 2-chloro or 4-chloro; (b) when R1 and R3 are hydrogen and R2 is 4-bromo or 4-chloro, then R4 may not be 4-chloro, 4-fluoro or 4-bromo; (c) when R1 and R3 are hydrogen and R2 is 4-fluoro, then R4 may not be 4-fluoro or 4-bromo; (d) when R1 is hydrogen, and R4 is 2-fluoro, the R2 and R3 may not be 4-fluoro; and (e) when R1 is hydrogen and R3 is 4- hydrogen, 4-chloro, 4-bromo, 4-methyl or 4-methoxy, and R4 is 2-hydrogen, 2-chloro, or 2-fluoro; then R2 may not be 4-hydrogen, 4-chloro, 4-fluoro, or 4-bromo.

les (E)-styryl benzylsulfones représentés par la formule (1) sont des agents anticancer. Dans cette formule R¿1?, R¿2?, R¿3?, et R¿4? sont indépendamment hydrogène, fluoro, chloro, iodo, bromo, C1-C6 alkyle, C1-C4 alcoxy, nitro, cyano et trifluorométhyle, sous réserve que (a) R¿1?, R¿2? et R¿3? ne soient pas tous hydrogène si R¿4? est chloro-2 ou chloro-4; (b) si R¿1? et R¿3? sont hydrogène et R¿2? est bromo-4 ou chloro-4, R¿4? ne peut être chloro-4, fluoro-4 ou bromo-4; (c) si R¿1? et R¿3? sont hydrogène et si R¿2? est fluoro-4, R¿4? ne peut pas être fluoro-4 ou bromo-4; (d) si R¿1? est hydrogène, et si R¿4? est fluoro-2, R¿2? et R¿3? ne peuvent pas être fluoro-4; et (e) si R¿1? est hydrogène et R¿3? est hydrogène-4, chloro-4, bromo-4, methyl-4 ou methoxy-4, et R¿4? est hydrogène-2, chloro-2, ou fluoro-2; R¿2? ne peut pas être hydrogène-4, chloro-4, fluoro-4, ou bromo-4.

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