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Molecules 2016, 21(11), 1534; doi:10.3390/molecules21111534

Oxoisoaporphine as Potent Telomerase Inhibitor

State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmacy, Guangxi Normal University, 15 Yucai Road, Guilin 541004, China
These authors contributed equally to this work.
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Author to whom correspondence should be addressed.
Academic Editor: Diego Muñoz-Torrero
Received: 4 September 2016 / Revised: 25 October 2016 / Accepted: 5 November 2016 / Published: 14 November 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [2411 KB, uploaded 14 November 2016]   |  

Abstract

Two compounds previously isolated from traditional Chinese medicine, Menispermum dauricum (DC), 6-hydroxyl-oxoisoaporphine (H-La), and 4,6-di(2-pyridinyl)benzo[h]isoindolo[4,5,6-de]quinolin-8(5H)-one (H-Lb), were known to have in vitro antitumor activity and to selectively bind human telomeric, c-myc, and bcl-2 G-quadruplexes (G4s). In this study, the binding properties of these two compounds to telomerase were investigated through molecular docking and telomeric repeat amplication protocol and silver staining assay (TRAP-silver staining assay). The binding energies bound to human telomerase RNA were calculated by molecular docking to be −6.43 and −9.76 kcal/mol for H-La and H-Lb, respectively. Compared with H-La, the ligand H-Lb more strongly inhibited telomerase activity in the SK-OV-3 cells model. View Full-Text
Keywords: oxoisoaporphine; telomerase; molecular docking oxoisoaporphine; telomerase; molecular docking
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MDPI and ACS Style

Wei, Z.-Z.; Qin, Q.-P.; Chen, J.-N.; Chen, Z.-F. Oxoisoaporphine as Potent Telomerase Inhibitor. Molecules 2016, 21, 1534.

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