Linked Life Data

20863599

Source:http://linkedlifedata.com/resource/pubmed/id/20863599

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
11
pubmed:dateCreated
2010-10-11
pubmed:abstractText
We have examined the antimalarial structure-activity relationship of a series of methoxylated chalcones (A-CHCH-CO-B) against Plasmodium falciparum (3D7 strain) using fluorescence-based SYBR Green assay. Our study has revealed that electron releasing methoxy groups on ring A and electron withdrawing groups on ring B increases antimalarial potency while the positional interchange of these groups causes a decrease. In particular, 2,4,5-trimethoxy substitution pattern at ring A provided potent analogues which were easily derived from abundantly available natural ?-asarone rich Acorus calamus oil. Cytotoxic evaluation indicated that the most active compounds 27 (IC(50): 1.8 ?M) and 26 (IC(50): 2 ?M) were also relatively non-toxic. Furthermore, compound 12 showed excellent resistance index of 1.1 against chloroquine resistant Dd2 strain of P. falciparum.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Nov
pubmed:issn
1768-3254
pubmed:author
pubmed:copyrightInfo
Copyright © 2010 Elsevier Masson SAS. All rights reserved.
pubmed:issnType
Electronic
pubmed:volume
45
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
5292-301
pubmed:meshHeading
pubmed:year
2010
pubmed:articleTitle
Reinvestigation of structure-activity relationship of methoxylated chalcones as antimalarials: synthesis and evaluation of 2,4,5-trimethoxy substituted patterns as lead candidates derived from abundantly available natural ?-asarone.
pubmed:affiliation
Natural Plant Products Division, Institute of Himalayan Bioresource Technology (C.S.I.R.), Palampur 176061, H.P., India.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't