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Selective anti-malarial minor groove binders.

Abstract：

:A set of 31 DNA minor groove binders (MGBs) with diverse structural features relating to both physical chemical properties and DNA binding sequence preference has been evaluated as potential drugs to treat Plasmodium falciparum infections using a chloroquine sensitive strain (3D7) and a chloroquine resistant strain (Dd2) in comparison with human embryonic kidney (HEK) cells as an indicator of mammalian cell toxicity. MGBs with an alkene link between the two N-terminal building blocks were demonstrated to be most active with IC50 values in the range 30-500nM and therapeutic ratios in the range 10->500. Many active compounds contained a C-alkylthiazole building block. Active compounds with logD7.4 values of approximately 3 or 7 were identified. Importantly the MGBs tested were essentially equally effective against both chloroquine sensitive and resistant strains. The results show that suitably designed MGBs have the potential for development into clinical candidates for antimalarial drugs effective against resistant strains of Plasmodia.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Scott FJ,Khalaf AI,Duffy S,Avery VM,Suckling CJ

doi

10.1016/j.bmcl.2016.05.039

subject

Has Abstract

pub_date

2016-07-15 00:00:00

pages

3326-3329

issue

14

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(16)30524-8

journal_volume

26

pub_type

杂志文章

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