Design and Synthesis of Peptide and Peptidomimetics Involved in Antiretroviral and Anticancer Therapies

Abstract Unit 1 The development of new anti-HIV-1 drugs is a global need, due to the resistance and the side effects arising from the therapies currently in use, for this reason we focused on an innovative target, the nucleocapsidic chaperonic protein(NC) of HIV-1 virus, which is involved in many steps of the virus replication, expecially the trascription. Moreover it plays a role of mediator in the annealing reaction of TAR with cTAR. 2,6-Dipeptidyl-anthraquinones are a promising class of nucleic acid-binding compounds that act as NC inhibitors in vitro. We designed, synthesized and tested new series of 2,6-disubstituted-anthraquinones, which are able to bind viral nucleic acid substrates of NC. We demonstrated that these novel derivatives interact preferentially with non-canonical structures of TAR and cTAR, stabilize their dynamics structures, such as bulge and loop, and interfere with NC chaperone activity.