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Synthesis and SAR of novel CXCR4 antagonists that are potent inhibitors of T tropic (X4) HIV-1 replication |
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| Authors: | Skerlj Renato Bridger Gary McEachern Ernie Harwig Curtis Smith Chris Wilson Trevor Veale Duane Yee Helen Crawford Jason Skupinska Krystyna Wauthy Rossana Yang Wen Zhu Yongbao Bogucki David Di Fluri Maria Langille Jonathon Huskens Dana De Clercq Erik Schols Dominique |
| Institution: | a Genzyme Corp., 153 Second Avenue, Waltham, MA 02451, USA b AnorMED, Inc., 200-20353 64th Avenue, Langley, British Columbia, Canada V2Y 1N5 c Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium |
| Abstract: | An early lead from the AMD070 program was optimized and a structure-activity relationship was developed for a novel series of heterocyclic containing compounds. Potent CXCR4 antagonists were identified based on anti-HIV-1 activity and Ca2+ flux inhibition that displayed good pharmacokinetics in rat and dog. |
| Keywords: | CXCR4 Chemokine receptor HIV AMD070 |
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