Aromatic hydroxylation by cytochrome P450: model calculations of mechanism and substituent effects

J Am Chem Soc. 2003 Dec 10;125(49):15004-5. doi: 10.1021/ja035590q.

Abstract

The mechanism and selectivity of aromatic hydroxylation by cytochrome P450 enzymes is explored using new B3LYP density functional theory computations. The calculations, using a realistic porphyrin model system, show that rate-determining addition of compound I to an aromatic carbon atom proceeds via a transition state with partial radical and cationic character. Reactivity is shown to depend strongly on ring substituents, with both electron-withdrawing and -donating groups strongly decreasing the addition barrier in the para position, and it is shown that the calculated barrier heights can be reproduced by a new dual-parameter equation based on radical and cationic Hammett sigma parameters.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cytochrome P-450 Enzyme System / chemistry*
  • Cytochrome P-450 Enzyme System / metabolism*
  • Hydrocarbons, Aromatic / chemistry*
  • Hydrocarbons, Aromatic / metabolism*
  • Hydroxylation
  • Models, Molecular
  • Thermodynamics

Substances

  • Hydrocarbons, Aromatic
  • Cytochrome P-450 Enzyme System