کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1396306 | 1501183 | 2010 | 10 صفحه PDF | دانلود رایگان |

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 β-asarone rich Acorus calamus oil. Cytotoxic evaluation indicated that the most active compounds 27 (IC50: 1.8 μM) and 26 (IC50: 2 μM) were also relatively non-toxic. Furthermore, compound 12 showed excellent resistance index of 1.1 against chloroquine resistant Dd2 strain of P. falciparum.
Chalcones (A–CHCH–CO–B) with 2,4,5-trimethoxy substitution pattern at ring A provided potent antimalarial analogues which were easily derived from abundantly available natural β-asarone rich Acorus calamus oil. Figure optionsDownload as PowerPoint slide
Journal: European Journal of Medicinal Chemistry - Volume 45, Issue 11, November 2010, Pages 5292–5301