Antiretroviral activity of metal-chelating HIV-1 integrase inhibitors.

作者: Mauro Carcelli , Dominga Rogolino , Mario Sechi , Gabriele Rispoli , Emilia Fisicaro

DOI: 10.1016/J.EJMECH.2014.06.055

关键词:

摘要: Data regarding the activity of metal complexes against HIV virus in cell are surprisingly scarce. In this study, we present antiviral HIV-infected cells different types chelating ligands and their complexes. particular, carboxamide scaffold corresponding coordination compounds demonstrated an interesting profile nanomolar range. These molecules inhibit not only integrase catalytic activity, but they also interfere with function RNase H component reverse transcriptase. Here discuss thermodynamic characterization solution most active ligands, affording to best our knowledge for first time type data anti-HIV activity.

参考文章(43)
Sharon L. Karmon, Martin Markowitz, Next-generation integrase inhibitors : where to after raltegravir? Drugs. ,vol. 73, pp. 213- 228 ,(2013) , 10.1007/S40265-013-0015-5
Elena A. Semenova, Christophe Marchand, Yves Pommier, HIV-1 integrase inhibitors: update and perspectives. Advances in pharmacology (San Diego). ,vol. 56, pp. 199- 228 ,(2008) , 10.1016/S1054-3589(07)56007-2
Brian A. Johns, Takashi Kawasuji, Jason G. Weatherhead, Teruhiko Taishi, David P. Temelkoff, Hiroshi Yoshida, Toshiyuki Akiyama, Yoshiyuki Taoda, Hitoshi Murai, Ryuichi Kiyama, Masahiro Fuji, Norihiko Tanimoto, Jerry Jeffrey, Scott A. Foster, Tomokazu Yoshinaga, Takahiro Seki, Masanori Kobayashi, Akihiko Sato, Matthew N. Johnson, Edward P. Garvey, Tamio Fujiwara, Carbamoyl Pyridone HIV-1 Integrase Inhibitors 3. A Diastereomeric Approach to Chiral Nonracemic Tricyclic Ring Systems and the Discovery of Dolutegravir (S/GSK1349572) and (S/GSK1265744) Journal of Medicinal Chemistry. ,vol. 56, pp. 5901- 5916 ,(2013) , 10.1021/JM400645W
Dominga Rogolino, Mauro Carcelli, Carlotta Compari, Laura De Luca, Stefania Ferro, Emilia Fisicaro, Gabriele Rispoli, Nouri Neamati, Zeger Debyser, Frauke Christ, Alba Chimirri, Diketoacid chelating ligands as dual inhibitors of HIV-1 integration process. European Journal of Medicinal Chemistry. ,vol. 78, pp. 425- 430 ,(2014) , 10.1016/J.EJMECH.2014.03.070
Lalintip Hocharoen, James A. Cowan, Metallotherapeutics: Novel Strategies in Drug Design Chemistry: A European Journal. ,vol. 15, pp. 8670- 8676 ,(2009) , 10.1002/CHEM.200900821
Brian A Johns, Angilique C Svolto, Advances in two-metal chelation inhibitors of HIV integrase Expert Opinion on Therapeutic Patents. ,vol. 18, pp. 1225- 1237 ,(2008) , 10.1517/13543776.18.11.1225
Roberta Costi, Mathieu Métifiot, Francesca Esposito, Giuliana Cuzzucoli Crucitti, Luca Pescatori, Antonella Messore, Luigi Scipione, Silvano Tortorella, Luca Zinzula, Ettore Novellino, Yves Pommier, Enzo Tramontano, Christophe Marchand, Roberto Di Santo, 6-(1-Benzyl-1H-pyrrol-2-yl)-2,4-dioxo-5-hexenoic acids as dual inhibitors of recombinant HIV-1 integrase and ribonuclease H, synthesized by a parallel synthesis approach. Journal of Medicinal Chemistry. ,vol. 56, pp. 8588- 8598 ,(2013) , 10.1021/JM401040B
John E. Ladbury, Gerhard Klebe, Ernesto Freire, Adding calorimetric data to decision making in lead discovery: a hot tip Nature Reviews Drug Discovery. ,vol. 9, pp. 23- 27 ,(2010) , 10.1038/NRD3054