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Salwa Elmeligie,Azza T. Taher,Nadia A. Khalil,Ahmed H. El-said 대한약학회 2017 Archives of Pharmacal Research Vol.40 No.1
Novel series of 1,3,4-trisubstituted azetidin-2-one derivatives 8a–p were synthesized and proposed ascytotoxic agents acting via inhibition of tubulin at thecolchicine binding site. The design of the target compoundswas based upon modification in the structure of the vasculartargeting agent combretastatin A-4 (CA-4). The cisdouble bond linker in CA-4 was replaced with the azetidin-2-one ring aiming to prevent the cis/trans isomerizationthat suppresses the activity of CA-4, thereby enhancing itsantiproliferative activity. All new compounds were investigatedin vitro against MCF-7 and HCT-116 cell lines. Theinhibition of tubulin polymerization by four most potentcompounds 8g, 8j, 8n and 8o was also evaluated. Thesynthesis of the final targets was achieved adopting Staudingerreaction. Molecular modeling studies were performedto rationalize the biological results.