Novel piperazine-1,2,3-triazole leads for the potential treatment of pancreatic cancer.

ABSTRACT: From lead 1, (N-(4-((4-(3-(4-(3-methoxyphenyl)-1H-1,2,3-triazol-1-yl)propyl)piperazin-1-yl)sulfonyl)-phenyl)acetamide), a S100A2-p53 protein-protein interaction inhibitor based on an in silico modelling driven hypothesis, four focused libraries were designed and synthesised. Growth inhibition screening was performed against 16 human cancer cell lines including the pancreatic cell lines MiaPaCa2, BxPC3, AsPC-1, Capan-2, HPAC, PANC-1 and the drug resistant CFPAC1. Modification of 1's phenylacetamide moiety, gave Library 1 with only modest pancreatic cancer activity. Modification of the 3-OCH₃Ph moiety (Library 2) gave 4-CH₃ (26), 4-CH₂CH₃ (27), 4-CF₃ (31) and 4-NO₂ (32) with sterically bulky

SUBMITTER: Sun J 

PROVIDER: S-EPMC10650957 | biostudies-literature | 2023 Nov

REPOSITORIES: biostudies-literature