Design, synthesis and biological evaluation of TAR and cTAR binders as HIV-1 nucleocapsid inhibitors

Alice Sosic; Francesco Frecentese; Elisa Perissutti; Laura Sinigaglia; Vincenzo Santagada; Giuseppe Caliendo; Elisa Magli; Antonio Ciano; Giuseppe Zagotto; Cristina Parolin; Barbara Gatto

doi:10.1039/C3MD00212H

Design, synthesis and biological evaluation of TAR and cTAR binders as HIV-1 nucleocapsid inhibitors†

Alice Sosic,^a Francesco Frecentese,^b Elisa Perissutti,^b Laura Sinigaglia,^a Vincenzo Santagada,^b Giuseppe Caliendo,^b Elisa Magli,^b Antonio Ciano,^b Giuseppe Zagotto,^a Cristina Parolin^c and Barbara Gatto*^a

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* Corresponding authors

^a Dipartimento di Scienze del Farmaco, Università di Padova, via Marzolo 5, Padova, Italy
E-mail: barbara.gatto@unipd.it

^b Dipartimento di Farmacia, Università degli Studi di Napoli “Federico II”, via D. Montesano 49, Napoli, Italy

^c Dipartimento di Biologia, Università di Padova, via U. Bassi 58/b, 35121 Padova, Italy

Abstract

We designed, synthesized and tested novel 2,6-disubstituted-anthraquinones able to bind dynamic secondary structures of nucleic acids, such as TAR RNA and its reverse transcript cTAR, leading to inhibition of the chaperone activities of the nucleocapsid NCp7, a highly conserved viral protein implied in crucial steps of HIV-1 replication.

MedChemComm

Design, synthesis and biological evaluation of TAR and cTAR binders as HIV-1 nucleocapsid inhibitors†

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Design, synthesis and biological evaluation of TAR and cTAR binders as HIV-1 nucleocapsid inhibitors

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