Cystargolide-based amide and ester Pz analogues as proteasome inhibitors and anti-cancer agents.
| Autor: | Viera CR; Department of Chemistry, New Mexico Institute of Mining and Technology, Socorro, NM 87801, USA., Stevens BT; Department of Biology, New Mexico Institute of Mining and Technology, Socorro, NM 87801, USA., Viera T; Department of Chemistry, New Mexico Institute of Mining and Technology, Socorro, NM 87801, USA., Zielinski C; Department of Chemical Engineering, New Mexico Institute of Mining and Technology, Socorro, NM 87801, USA., Uranga LA; Department of Chemistry and Biochemistry, New Mexico State University, Las Cruces, NM 88003, USA., Rogelj S; Department of Biology, New Mexico Institute of Mining and Technology, Socorro, NM 87801, USA., Patidar PL; Department of Chemistry, New Mexico Institute of Mining and Technology, Socorro, NM 87801, USA., Tello-Aburto R; Department of Chemistry and Biochemistry, New Mexico State University, Las Cruces, NM 88003, USA. |
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| Jazyk: | angličtina |
| Zdroj: | Royal Society open science [R Soc Open Sci] 2022 Sep 28; Vol. 9 (9), pp. 220358. Date of Electronic Publication: 2022 Sep 28 (Print Publication: 2022). |
| DOI: | 10.1098/rsos.220358 |
| Abstrakt: | A series of cystargolide-based β-lactone analogues containing nitrogen atoms at the Pz portion of the scaffold were prepared and evaluated as proteasome inhibitors, and for their cytotoxicity profile toward several cancer cell lines. Inclusion of one, two or even three nitrogen atoms at the Pz portion of the cystargolide scaffold is well tolerated, producing analogues with low nanomolar proteasome inhibition activity, in many cases superior to carfilzomib. Additionally, analogue 8g , containing an ester and pyrazine group at Pz, was shown to possess significant activity toward RPMI 8226 cells (IC (© 2022 The Authors.) |
| Databáze: | MEDLINE |
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