Study On The Design, Synthesis And Antitumor Activity Of WB852 Analogues

WB852,one of the representatives of 2-alkylaminomethyl-5-(E)-alkylidene cyclopentanone hydrochlorides possessing antineoplamic activity,showed enough advantages and potentials in widely studies.This paper exactly deals with the optimization of WB852.While proceeding on our research,naturally occurring Melodorinol timely illuminate us for three series of structurally novel target compounds:(E)-5-[(3-dimethylaminomethyl-2-oxo)cyclopentylidene]pentyl benzonates or cinnamates hydrochlorides,N-(E)-5-[(3-dimethylaminomethyl-2-oxo)cyclopentylidene]pentyl benzarnides or cinnamides hydrochlorides and(E)-2-hydroxyl or acetyhydroxyl-3-[(3-dimethyl-arninomethyl-2-oxo) cyclopentylidene]propyl benzoate hydrochlorides.Starting from cyelopentanone and hydroxypentanal,following Aldol reaction,Gabriel reaction,Mannich reaction and other procedures,we got 20 compounds of seriesâ… and 3 compounds of seriesâ…¡.Starting from cyclopentanone and mannitol 2 key intermediates of seriesâ…¢were obtained.All the synthesized compounds were characterized by ~1H-NMR and MS.Finally,the antineoplamic activities of some synthesized compounds were tested by the MTT method in vitro against PC-3(Human Prostate Cancer) which is able to generate some intelligence about SARs.