2. Academic Validation
  3. The synthesis of 4,6-diaryl-2-pyridones and their bioactivation in CYP1 expressing breast cancer cells

The synthesis of 4,6-diaryl-2-pyridones and their bioactivation in CYP1 expressing breast cancer cells

  • Bioorg Med Chem Lett. 2019 Jun 1;29(11):1403-1406. doi: 10.1016/j.bmcl.2019.03.030.
Ketan C Ruparelia 1,  Sabahat Lodhi 1,  Dyan N Ankrett 1,  Nicola E Wilsher 1,  Randolph R J Arroo 1,  Gerard A Potter 1,  Kenneth J M Beresford 2
Affiliations

Affiliations

  • 1 Leicester School of Pharmacy, Faculty of Health and Life Sciences, De Montfort University, The Gateway, Leicester LE1 9BH, UK.
  • 2 Leicester School of Pharmacy, Faculty of Health and Life Sciences, De Montfort University, The Gateway, Leicester LE1 9BH, UK. Electronic address: kberesford@dmu.ac.uk.
PMID: 30935796 DOI: 10.1016/j.bmcl.2019.03.030
Abstract

As part of a programme to develop Anticancer prodrugs which are activated by Cytochrome P450 (CYP)1B1, a library of 4,6-diaryl-2-pyridones was synthesised in yields of 6-60% from the corresponding Chalcones. A number of these derivatives showed promising antiproliferative activities in human breast Cancer cell lines which express CYP1B1 and CYP1A1, while showing little toxicity towards a non-tumour breast cell line with no CYP expression. Metabolism studies provided evidence supporting the involvement of CYP1 Enzymes in the bioactivation of these compounds.

Keywords

4,6-Diaryl-2-pyridones; Antiproliferative; CYP1B1; Chalcones; Prodrug.

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