Design, Synthesis, and Biological Evaluation of 1,3-Diarylpropenones as Dual Inhibitors of HIV-1 Reverse Transcriptase (pages 1869–1879)
Dr. Rita Meleddu, Dr. Valeria Cannas, Dr. Simona Distinto, Dr. Giorgia Sarais, Dr. Claudia Del Vecchio, Dr. Francesca Esposito, Dr. Giulia Bianco, Dr. Angela Corona, Dr. Filippo Cottiglia, Prof. Stefano Alcaro, Prof. Cristina Parolin, Dr. Anna Artese, Dr. Daniela Scalise, Prof. Massimo Fresta, Dr. Antonella Arridu, Dr. Francesco Ortuso, Prof. Elias Maccioni and Prof. Enzo Tramontano
Version of Record online: 21 MAY 2014 | DOI: 10.1002/cmdc.201402015
1,3-Diarylpropenones were synthesized and assayed for their activity toward HIV-1 reverse transcriptase (RT). Dual inhibition properties in the low-micromolar range were observed, and mutations in the RT binding pocket were found to have an interesting effect on inhibition. Biochemical and computational approaches were applied with an aim to understand the possible mechanism of action.