Jatrophane diterpenes as modulators of multidrug resistance. Advances of structure-activity relationships and discovery of the potent lead pepluanin A.

@article{Corea2004JatrophaneDA,
  title={Jatrophane diterpenes as modulators of multidrug resistance. Advances of structure-activity relationships and discovery of the potent lead pepluanin A.},
  author={Gabriella Corea and Ernesto Fattorusso and Virginia Lanzotti and Riccardo Motti and Pierre-No{\"e}l Simon and Charles Dumontet and Attilio di Pietro},
  journal={Journal of medicinal chemistry},
  year={2004},
  volume={47 4},
  pages={988-92}
}
From the whole plant of Euphorbia peplus L., five new diterpenes based on a jatrophane skeleton (pepluanins A-E, 1-5) were isolated, together with two known analogues (6 and 7), which served to divulge in detail the structure-activity relationships within this class of P-glycoprotein inhibitors. The results revealed the importance of substitutions on the medium-sized ring (carbons 8, 9, 14, and 15). In particular, the activity is collapsed by the presence of a free hydroxyl at C-8, while it… CONTINUE READING

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