Evaluation of bisindole as potent β-glucuronidase inhibitors: Synthesis and in silico based studies
2014; Elsevier BV; Volume: 24; Issue: 7 Linguagem: Inglês
10.1016/j.bmcl.2014.02.015
ISSN1464-3405
AutoresKhalid Mohammed Khan, Fazal Rahim, Abdul Wadood, Muhammad Taha, Momin Khan, Shagufta Naureen, Nida Ambreen, Shafqat Hussain, Shahnaz Perveen, M. Iqbal Choudhary,
Tópico(s)Synthesis and biological activity
ResumoBisindole analogs 1–17 were synthesized and evaluated for their in vitro β-glucuronidase inhibitory potential. Out of seventeen compounds, the analog 1 (IC50 = 1.62 ± 0.04 μM), 6 (IC50 = 1.86 ± 0.05 μM), 10 (IC50 = 2.80 ± 0.29 μM), 9 (IC50 = 3.10 ± 0.28 μM), 14 (IC50 = 4.30 ± 0.08 μM), 2 (IC50 = 18.40 ± 0.09 μM), 19 (IC50 = 19.90 ± 1.05 μM), 4 (IC50 = 20.90 ± 0.62 μM), 7 (IC50 = 21.50 ± 0.77 μM), and 3 (IC50 = 22.30 ± 0.02 μM) showed superior β-glucuronidase inhibitory activity than the standard (d-saccharic acid 1,4-lactone, IC50 = 48.40 ± 1.25 μM). In addition, molecular docking studies were performed to investigate the binding interactions of bisindole derivatives with the enzyme. This study has identified a new class of potent β-glucouronidase inhibitors.
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