Alkylated monoterpene indole alkaloid derivatives as potent P-glycoprotein inhibitors in resistant cancer cells

Aza-tryptamine substrates in monoterpene indole alkaloid biosynthesis.

Biosynthetic pathways can be hijacked to yield novel compounds by introduction of novel starting materials. Here we have altered tryptamine, which serves as the starting substrate for a variety of alkaloid biosynthetic pathways, by replacing the indole with one of four aza-indole isomers. We show that two aza-tryptamine substrates can be successfully incorporated into the products of the monote...

Chemistry and biology of monoterpene indole alkaloid biosynthesis.

Aureobasidins as new inhibitors of P-glycoprotein in multidrug resistant tumor cells.

Cyclic depsipeptide antibiotic aureobasidin A (AbA) and its analogs were tested for the inhibitory activity of P-glycoprotein in multidrug resistant cancer cells as well as for the antifungal activity. Some analogs with lower antifungal activity than AbA showed higher inhibition of P-glycoproteins indicating difference of the structure-activity relationships between the two activities. Among Ab...

quantitative structure activity relationship and docking studies on imidazole derivatives as p-glycoprotein inhibitors

Phloroglucinol Derivatives as Potent Photosystem II Inhibitors

Studies on structure/activity relationships o f phloroglucinol derivatives tha t had been de­ signed based on the structures o f grandinol and hom ograndinol. potent photosystem II (PS II) inhibitors in Eucalyptus grandis, revealed th a t two electron-withdraw ing groups which differ by their electron-w ithdraw ing pow er on a phloroglucinol nucleus were essential for activity. A larger differe...