New oseltamivir analogues were designed and synthesized, starting from shikimic acid. Biological evaluation against three human cancer cell lines (KB, MCF7 and Lu-1) showed that many of them exhibited cytotoxic activity. Azides 5 are more active than the corresponding amines 6. Thus, the reduction of the azide group into amine led to the loss of cytotoxicity. The compounds with a cyclohexanemethyloxy group at C-3 were more active than the other investigated compounds belonging to the same series. This cyclohexanemethyloxy group seems to be critical for the cytotoxic activity of this class of compounds. The synthetic oseltamivir analogues 6a-e had no inhibition activity, even at the concentration of 50 µM when they were evaluated for their in vitro influenza A neuraminidase inhibitory activity by an enzymatic assay.
Canna edulis
Ker rhizome has been used in Traditional Vietnamese Medicine to prevent and treat heart diseases without thorough scientific evidence. The data presented in this article characterize the antiplatelet aggregation, anticoagulant and antioxidant activity of
C. edulis
rhizome extracts and the bio-guided isolation of bioactive compounds from the active fraction. The data on tested bioactivities of isolated compounds were also provided. The inhibitory effect on adenosine diphosphate- and collagen-induced human platelet aggregation was evaluated through three parameters: percentage inhibition of platelet aggregation, aggregation velocity and area under the platelet aggregation curve. Prothrombin time, activated partial thromboplastine time and thrombine time were measured to examine the anticoagulant activity. The free radical scavenging ability was assessed with DPPH and ABTS assays. The structures of compounds were elucidated by NMR and MS spectroscopic methods. The data showed that the ethyl acetate fraction showed the most potent antiplatelet aggregation, anticoagulant and antioxidant activity. Seven known compounds: 5-hydroxy-6-methyl-2
H
-pyran-2-one
(1)
, epimedokoreanone A
(2)
, nepetoidin B
(3)
, ferulic acid
(4)
, caffeic acid
(5)
, hydroxytyrosol
(6)
, and 1H-indole-3-carboxaldehyde
(7)
were isolated from this active fraction. Moreover, this article provided experimental data on antiplatelet effect of epimedokoreanone A
(2)
and nepetoidine B
(3)
, anticoagulant and antioxidant activity of epimedokoreanone A
(2)
and also antiplatelet and antioxidant activity of 5-hydroxy-6-methyl-2
H
-pyran-2-one
(1)
.
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