Synthesis of new non peptidic inhibitors of HIV Protease antivirals bearing heteroaromatic fragments and evaluation of their "repurposing" as antitumor compounds Line of research The research activity concerns the synthesis of molecules bearing an heteroaromatic fragment on an hydroxyethylamine core, starting from enantiopure epoxides, easily available from chiral pool and their evaluation as non peptidic inhibitors of HIV Protease (native or mutate), together with their repurposing as antitumor compounds. Regioselective oxiranyl ringopening reactions and selective functionalization of amine groups are studied. Tests of their in vitro and ex vivo (in cells) activity are made in collaboration with the University of Trieste and University of Basilicata. Staff Supervisor: Paolo Lupattelli Publications Two Novel Precursors of the HIV-1 Protease Inhibitor Darunavir Target the UPR/Proteasome System in Human Hepatocellular Carcinoma Cell Line HepG2The Pseudo-Symmetric N-benzyl Hydroxyethylamine Core in a New Series of Heteroarylcarboxyamide HIV-1 Pr Inhibitors: Synthesis, Molecular Modeling and Biological EvaluationNew heteroaryl carbamates: Synthesis and biological screening in vitro and in mammalian cells of wild-type and mutant HIV-protease inhibitorsSynthesis and biological evaluation in vitro and in mammalian cells of new heteroaryl carboxyamides as HIV-protease inhibitors Theme and ERC Theme: Life-Sciences chemistryERC: LS1_1 Molecular interactionsPE4_3 Molecular architecture and StructurePE5_17 Organic chemistry Traineeship offer Area di ricerca: Organic chemistryAvailability: one positionCourse of study (advised): ChemistryIndustrial chemistry
