Biological and Medicinal Chemistry

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



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.


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Supplementary material

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