Discovery and synthesis of novel luteolin derivatives as DAT agonists.

Abstract:

:Luteolin, 5,7-dihydroxy-2-(3,4-dihydroxyphenyl)-4H-chromen-4-one, has been proposed and proved to be a novel dopamine transporter (DAT) activator. In order to develop this potential of luteolin, a series of novel luteolin derivatives were designed, synthesized, and evaluated for their DAT agonistic activities, utilizing constructed Chinese hamster ovary (CHO) cell lines stably expressing rat DAT. Biological screening results demonstrated that luteolin derivatives 1d, 1e, and 4c carry great DAT agonistic potency (EC(50)=0.046, 0.869, and 1.375μM, respectively) compared with luteolin 8 (EC(50)=1.45±0.29μM). Luteolin derivative 1d, notably, exhibited a 32-fold-higher DAT agonistic potency than luteolin. These luteolin derivatives represent a novel DAT agonist class, from which lead compounds useful for exploration of additional novel DAT agonists could be drawn.

journal_name

Bioorg Med Chem

authors

Zhang J,Liu X,Lei X,Wang L,Guo L,Zhao G,Lin G

doi

10.1016/j.bmc.2010.09.049

subject

Has Abstract

pub_date

2010-11-15 00:00:00

pages

7842-8

issue

22

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(10)00886-2

journal_volume

18

pub_type

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