1198088-63-9Relevant articles and documents
The synthesis of 4,6-diaryl-2-pyridones and their bioactivation in CYP1 expressing breast cancer cells
Ruparelia, Ketan C.,Lodhi, Sabahat,Ankrett, Dyan N.,Wilsher, Nicola E.,Arroo, Randolph R.J.,Potter, Gerard A.,Beresford, Kenneth J.M.
, p. 1403 - 1406 (2019/04/01)
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.
4, 6-DIPHENYLPYRID-2-0NES AGAINST CANCER
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Page/Page column 23, (2009/12/28)
A compound for use in the treatment of proliferative disorders, such as cancer, having the following formula:z wherein: R1, R2 and R3 are independently H or lower alkyl; R4, R5, R6, R7 and R8 are independently H, halo, lower alkyl or -O-lower alkyl, provided that at least one is -O-lower alkyl; or at least one pair of R4 to R8, the members of which pair are adjacent to one another on the ring, are conjoined to form-0-(CR14R15)n-O-, where n is 1 or 2 and R14 and R15 are independently H or lower alkyl, and the remainder of R4 to R8 are independently H, halo, lower alkyl or -O-lower alkyl; and R9, R10, R11, R12 and R13 are independently H, halo, lower alkyl or -O-lower alkyl, provided that at least one is -O-lower alkyl; or at least one pair of R9 to R13, the members of which pair are adjacent to one another on the ring, are conjoined to form-O-(CR16R17)m-O-, where m is 1 or 2 and R16 and R17 are independently H or lower alkyl, and the remainder of R9 to R13 are independently H, halo, lower alkyl or -O-lower alkyl.