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Some compounds are much less toxic than the natural product febrifugine and existing antimalarial drugs and are expected to possess wide therapeutic windows.
The aromatase inhibitory activities of these compounds are much more potent than that for the lead compound resveratrol, which has an IC50 of 80 μM.
Some compounds are much less toxic than the natural product febrifugine and existing antimalarial drug chloroquine and are expected to possess wide therapeutic windows.
Disulfides and diselenides are far more stable than peroxides, and sulfonium and selenonium salts are much less reactive than oxonium salts; at the same time, simple thiocarbonyl (C=S) and selenocarbonyl (C=Se) compounds are much more reactive than simple carbonyl (C=O) compounds.
General SAR has been established for the substituents at positions 1 and 2, as well as the importance of the ethylene group and its attachment to position 5. Optimized compounds are much more potent than SAHA in both enzymatic and cellular assays.
1-O-[(3′S,4′R -3-hydroxytetrahydrofuran-4-yl 3′S,4′R -3-hydroxytetrahydrofuran-4-yl 3′S,4′R -3-hydroxytetrahydrofuran-4-yl 3′S,4′R -3-hydroxytetrahydrofuran-4-yl 3′S,4′R -3-hydroxytetrahydrofuran-4-yl′S)-3-hydroxytetrahydrofuran-4-yl] β-d-xylopyranoside 3,4,3′-trisphosphate, is ca. 20-fold weaker than Ins(1,4,5)P3, and the other compounds are much less active.
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The compounds were much less potent on mammalian protein prenyltransferases.
Biologically, FONs-photosensitizers from these compounds were much more phototoxicities to cancer cell than to normal cell without significant dark toxicity.
In addition, the microhardness values of the Mg Al Zn intermetallic compounds were much higher than those of the substrate and this would greatly contribute to the enhancement of wear resistance.
This response was clearly synergistic since the increase in the levels of these compounds was much greater in the presence of both elicitors than when they were used separately.
Cytotoxicity against HPAC cell line was evaluated, and two of them exhibited comparable potency to kazusamycin A. Hepatic toxicity of these designed compounds was much lower than that of kazusamycin A.
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