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Synthesis and biological activity of alpha-bromoacryloyl lexitropsin conjugates

Romagnoli, Romeo ; Baraldi, Pier Giovanni ; Iaconinoto, Maria Antonietta ; Carrion, Maria Dora ; Tabrizi, Mojgan Aghazadeh ; Gambari, Roberto ; Borgatti, Monica ; Heilmann, Jörg


The design, synthesis and biol. evaluation of lexitropsins bearing mixed heterocyclic and benzoheterocyclic moieties and tethered to an alpha-bromo acrylic moiety acting as alkylating moiety are reported, and structure-activity relationships detd. For example, indolecarboxylic acid I reacted with pyrrole deriv. II to give analog III (X = Y = CH, Z = NMe) in 63% yield. With respect to ...


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