Synthetic molecules designed as potential inhibitors in ecdysone biosynthesis

For fundamental studies as well as applied research, we have set up a programme for the synthesis of irreversible and selective inhibitors of ecdysone biosynthesis. Suicide substrate type inhibitors have been synthesized in order to react in the last steps of ecdysone biosynthesis on C‐22 and C‐25 hydroxylases which are cytochrome P‐450‐dependent monooxygenases. The most active inhibitors are formed of a steroid nucleus on which a short side chain, with an acetylenic or an allenic function closely linked to an hydroxyl group, has been grafted. The exact form of the steroid nucleus (as in cholesterol, 7‐dehydrocholesterol, 3‐dehydrocholesterol or a molecule with a saturated B cycle) did not appear essential for the activity of the chemicals. These molecules injected in vivo in larvae of Locusta migratoria induced some morphological modifications of the adults and a very slight delay in metamorphosis.

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