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Optimization of anti-proliferative activity using a screening approach with a series of bis-heterocyclic G-quadruplex ligands.

Abstract：

:Using a phenotypic screening and SAR optimization approach, a phenyl-bis-oxazole derivative has been identified with anti-proliferative activity, optimized with the use of a panel of cancer cell lines. The lead compound was synthesized by means of a short and effective two-step synthesis using Pd-catalyzed direct arylation. The compound stabilizes several quadruplex DNA sequences including a human telomeric DNA and one from the promoter of the HSP90 gene, although the structure-activity relationships of the series are not obviously related to the quadruplex binding.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Ohnmacht SA,Ciancimino C,Vignaroli G,Gunaratnam M,Neidle S

doi

10.1016/j.bmcl.2013.07.057

subject

Has Abstract

pub_date

2013-10-01 00:00:00

pages

5351-5

issue

19

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)00902-5

journal_volume

23

pub_type

杂志文章

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