Abstract
Argentatins A–C (1–3), the major cycloartane-type triterpenoids of guayule resin, a byproduct of commercial rubber production, were converted into their pyrimidine (7–12), thiazole (13–15), and indole (16–18) analogues by a molecular hybridization approach. The cytotoxic activities of these fused heterocyclic analogues 7–18 were compared with those of argentatins A–C (1–3) against a panel of three sentinel human cancer cell lines [NCI-H460 (non-small cell lung), MCF-7 (breast adenocarcinoma), and SF-268 (central nervous system glioma)], and normal human fibroblast (WI-38) cells. The cytotoxicity data suggest that the pyrimidine analogues 7 and 8 (derived from 1), 9 and 10 (derived from 2), and 12 (derived from 3) had significantly enhanced activity compared to the parent compounds or their thiazole (13–15) and indole (16–18) analogues. These findings indicate that triterpenoid constituents of guayule resin may be exploited to obtain value-added products with potential applications in anticancer drug discovery.
Highlights
Natural products (NPs) continue to be valuable sources of structurally diverse and biologically active compounds for drug discovery [1,2,3]
We report the semi-synthesis of novel pyrimidine, thiazole, and indole analogues 7–18 of argentatins A–C (1–3) and the investigation of their cytotoxic activity against three sentinel human cancer cell lines and normal human fibroblast cells
All analogues were evaluated for their cell proliferation inhibitory activity against the three sentinel cancer cell lines NCIH460, MCF-7, SF-268, and towards normal fibroblast cells, WI-38
Summary
Natural products (NPs) continue to be valuable sources of structurally diverse and biologically active compounds for drug discovery [1,2,3].
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