The design and the synthesis of new self-assembling conjugates is reported. The target compounds are characterized by the presence of a self-immolative linker that secures a controlled release induced by lipase cleavage. 4-(1,2-Diphenylbut-1-en-1-yl)aniline is used as a self-assembling inducer and amino-thiocolchicine as prototype of drug. The release of thiocolchicine derivative has been demonstrated in vitro in the presence of porcine pancreatic lipase (PPL) and celite-supported lipase (PS). The formation of nanoparticles is confirmed by DLS, atomic force microscopy (AFM) and fluorescence microscopy. The antiproliferative activity has been proved on two human cancer cell lines.
Self-assembling Releasable Thiocolchicine-Diphenylbutenylaniline Conjugates
2019
Abstract
The design and the synthesis of new self-assembling conjugates is reported. The target compounds are characterized by the presence of a self-immolative linker that secures a controlled release induced by lipase cleavage. 4-(1,2-Diphenylbut-1-en-1-yl)aniline is used as a self-assembling inducer and amino-thiocolchicine as prototype of drug. The release of thiocolchicine derivative has been demonstrated in vitro in the presence of porcine pancreatic lipase (PPL) and celite-supported lipase (PS). The formation of nanoparticles is confirmed by DLS, atomic force microscopy (AFM) and fluorescence microscopy. The antiproliferative activity has been proved on two human cancer cell lines.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
