Synthesis and preliminary biological evaluation of 6-O-[11C]-[(methoxymethyl)benzyl]guanines, new potential PET breast cancer imaging agents for the DNA repair protein AGT

Bioorg Med Chem Lett. 2003 Feb 24;13(4):641-4. doi: 10.1016/s0960-894x(02)01048-x.

Abstract

Novel radiolabeled O(6)-benzylguanine derivatives, 6-O-[(11)C]-[(methoxymethyl)benzyl]guanines ([(11)C]p-O(6)-MMBG, 1a; [(11)C]m-O(6)-MMBG, 1b; ([(11)C]o-O(6)-MMBG, 1c), have been synthesized for evaluation as new potential positron emission tomography (PET) breast cancer imaging agents for DNA repair protein, O(6)-alkylguanine-DNA alkyltransferase (AGT).

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Breast Neoplasms / diagnosis
  • Breast Neoplasms / diagnostic imaging*
  • Cell Line, Tumor
  • Enzyme Inhibitors* / chemical synthesis
  • Guanine / analogs & derivatives*
  • Guanine / chemical synthesis
  • Humans
  • O(6)-Methylguanine-DNA Methyltransferase / antagonists & inhibitors*
  • O(6)-Methylguanine-DNA Methyltransferase / metabolism
  • Protein Binding
  • Structure-Activity Relationship
  • Tomography, Emission-Computed / methods*

Substances

  • Enzyme Inhibitors
  • Guanine
  • O(6)-Methylguanine-DNA Methyltransferase