Lipophilic Salirasib analogs with enhanced antiproliferative activity against human solid tumor cell lines

15 September 2021, Version 1
This content is a preprint and has not undergone peer review at the time of posting.


Aim: We proposed to determine the antiproliferative activity of a series of synthetic salirasib analogs, presenting or not a 1,2,3-triazole linker, against five different cancer cell lines. Results: Bioassay, cheminformatic, and in silico ADME-Tox allowed the identification of new potent analogs. SAR analysis allowed the identification of structural and physicochemical features that benefit the antiproliferative activity. Conclusion: Isoprenyl R chains with three or more isoprene units, or long aliphatic R chains are the preferred ones within the active compounds. Likewise, we have identified three compounds with better activity profiles than salirasib against all the cell lines tested.


SAR studies

Supplementary materials

Supporting information - biological assays and chemoimformatics
General procedure for in vitro antiproliferative activity. In silico Physicochemical properties prediction. SAR analysis. ADMETox.


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