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Synthesis and molecular docking study of novel coumarin derivatives containing 4,5-dihydropyrazole moiety as potential antitumor agents.

Abstract：

: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 IC(50) 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 IC(50) 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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Liu XH,Liu HF,Chen J,Yang Y,Song BA,Bai LS,Liu JX,Zhu HL,Qi XB

doi

10.1016/j.bmcl.2010.08.017

subject

Has Abstract

pub_date

2010-10-01 00:00:00

pages

5705-8

issue

19

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)01140-6

journal_volume

20

pub_type

杂志文章

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