. 2016 Jan 20;7(3):324–329. doi: 10.1021/acsmedchemlett.5b00472

Table 1. Trp23 Substitution Structure–Activity Relationships^a.

graphic file with name ml-2015-00472u_0012.jpg

graphic file with name ml-2015-00472u_0013.jpg

Biochemical p53-HDM2 binding fluorescent polarization (FP) assay and antiproliferative osteosarcoma SJSA-1 assay results for compounds 3–14. Fluorescence polarization (FP) peptide displacement assay value was determined as described in Zhang et al.¹⁵ For comparison Nutlin-3a fluorescence polarization (FP) peptide displacement IC₅₀ assay value obtained in house was 0.07 μM. In our antiproliferative assay, Nutlin-3a had an IC₅₀ value of 1.9 μM using osteosarcoma SJSA-1 cells.

Racemic mixture.

Allyl group at position 2 of piperidine.

Phenoxybutanoic acid side chain.

Table 1. Trp23 Substitution Structure–Activity Relationshipsa.

Table 1. Trp23 Substitution Structure–Activity Relationships^a.