| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1362963 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
A series of novel coumarin derivatives containing 4,5-dihydropyrazole moiety as potential telomerase inhibitors were synthesized. The bioassay tests show that compound 3d exhibited potentially high activity against human gastric cancer cell SGC-7901 with IC50 value of 2.69 ± 0.60 μg/mL. All title compounds were assayed for telomerase inhibition by a modified TRAP assay, the results show that compounds 3d and 3f can strongly inhibit telomerase with IC50 values of 2.0 ± 0.07 and 1.8 ± 0.35 μM, respectively. Docking simulation was performed to position compound 3d into the telomerase (3DU6) active site to determine the probable binding model.
Graphical abstractNovel coumarin derivatives containing 4,5-dihydropyrazole moiety as potential telomerase inhibitors were synthesized. The bioassay tests showed that compound 3d exhibited potentially high activity against human gastric cancer cell SGC-7901 with the IC50 value was 2.69 ± 0.60 μg/mL.Figure optionsDownload full-size imageDownload as PowerPoint slide
