Antiproliferative Effect of Indole Phytoalexins

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Antiproliferative Effect of Indole Phytoalexins.

Indole phytoalexins from crucifers have been shown to exhibit significant anti-cancer, chemopreventive, and antiproliferative activity. Phytoalexins are natural low molecular antimicrobial compounds that are synthesized and accumulated in plants after their exposure to pathogenic microorganisms. Most interestingly, crucifers appear to be the only plant family producing sulfur-containing indole ...

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The synthesis and biological evaluation of a series of novel heterocyclic indole derivatives is described. The consolidation of the combretastatin and bisindolylmaleimide templates towards the inclusion of a novel heterocyclic ring proffered a versatile pharmacophore with which to pursue chemical diversification. Given literature precedent, maleimide was initially investigated in this role and ...

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Growth inhibitions on human cancer cell cultures with the indole sulphur-containing phytoalexins and their analogues.

Cell growth inhibitions on human cancer cell cultures were determined for the indole sulphur-containing phytoalexins cyclobrassinin, brassilexin (previously isolated from vegetables of the Cruciferae family) and their synthetic analogues 5-methoxybrassilexin and homocyclobrassinin. The most biologically active of these products is brassilexin (LD50 = 8 micrograms/ml).

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Toxins could be effective anticancer drugs, if their selective delivery into cancer cells could be achieved. We have shown that the energy of membrane-associated folding of water-soluble membrane peptides of the pHLIP (pH low insertion peptide) family could be used to move cell-impermeable cargo across the lipid bilayer into the cytoplasm of cancer cells. Here we present the results of a study ...

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ژورنال

عنوان ژورنال: Molecules

سال: 2016

ISSN: 1420-3049

DOI: 10.3390/molecules21121626