Bioorganic and Medicinal Chemistry Letters p. 1403 - 1406 (2019)
Update date:2022-08-03
Topics:
Ruparelia, Ketan C.
Lodhi, Sabahat
Ankrett, Dyan N.
Wilsher, Nicola E.
Arroo, Randolph R.J.
Potter, Gerard A.
Beresford, Kenneth J.M.
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.
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