Structure activity studies on the crinane alkaloid apoptosis-inducing pharmacophore. Academic Article uri icon

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abstract

  • The apoptosis-inducing ability of alpha-ethano bridged crinane alkaloids was investigated using natural and semi-synthetic derivatives uncovering novel structural requirements of this cytotoxic pharmacophore. An alpha-ethano bridge is required; an alpha- or beta-methoxy or hydroxyl H-bond acceptor are all tolerated at C-3; a small substituent (H, or OH) alone is tolerated at C-11; and a C-1 to C-2 double bond is shown to modulate, but is not a requirement for, apoptosis-inducing activity.

authors

  • Mcnulty, James
  • Nair, Jerald J
  • Bastida, Jaume
  • Pandey, Siyaram
  • Griffin, Carly

publication date

  • April 2009