| 摘要 |
<p>The invention is concerned with phorboid derivatives of the formula: P o - S o - E o wherein P o represents a radical formally derived from a parent compound which (a) binds reversibly or irreversibly to a diacylglycerol-type receptor; and/or (b) activates any form of the enzyme protein kinase C; and (c) contains an hydroxymethyl or 1-hydroxyethyl group bonded to a carbon atom; and wherein S o-E o represents a moiety which is either i) singly or doubly bonded to the carbon atom of the parent compound in place of the hydroxymethyl or 1-hydroxyethyl group; or ii) singly or doubly bonded to a carbon immediately adjacent to the carbon atom to which the hydroxymethyl or 1-hydroxyethyl; and wherein S o is a saturated or unsaturated, straight or branched chain of atoms which separates P o and E o by a linear count of at least two but not more than 6 atoms and contains one to six heteroatoms selected from oxygen, nitrogen and sulfur, a phosphorus atom, or up to 12 halogen atoms; provided that the total number of atoms does not exceed about 35; and wherein E o comprises a saturated or singly or multiply unsaturated group containing up to 8 carbon atoms and optionally containing 1 to 12 halogen atoms, 1 to 4 heteroatoms selected independently from oxygen, nitrogen and sulfur and one phosphorus atom, or wherein S o E o taken together may be a hydrogen, halogen, or ketonic oxygen atom or a hydroxy, amine, or thiol group singly or doubly bonded to the carbon atom of the parent compound P o in place of the hydroxymethyl or 1-hydroxyethyl group. The phorboid derivatives according to the invention block the toxic effects of the hydroxymethylcontaining phorboids and lack the toxic properties of previously available phorboids.</p> |
