Amino alcohol acrylonitriles as broad spectrum and tumour selective cytotoxic agents.

ABSTRACT: We have identified specific dichlorophenylacrylonitriles as lead compounds in the development of novel anticancer compounds, notably, (Z)-N-(4-(2-cyano-2-(3,4-dichlorophenyl)vinyl)phenyl)acetamide (1) and ANI-7 (2). Herein we specifically probe the SAR associated with the terminal aromatic ring and associated cytoxicity in a broad range of human cancer cell lines. Synthesis of three focused libraries revealed a poor tolerance for electron withdrawing and donating moieties (Library A). A clear preference for hydrophobic substituents on a terminal piperazine moiety (Library B) with good levels of broad spectrum cytotoxicity, e.g. 13a (GI₅₀ 2.5-6.0 μM), as did the introduction of a methylene spacer with 13i (4-CH₃PhCH

SUBMITTER: Baker JR 

PROVIDER: S-EPMC8223738 | biostudies-literature | 2021 Jun

REPOSITORIES: biostudies-literature