Synthesis and biological screening of a library of macamides as TNF-α inhibitors.

ABSTRACT: Thirty-five macamide analogues were synthesised by modifying the initial molecular structure. The resulting structures were confirmed using NMR and MS. Cytotoxicity and the anti-inflammatory activity of these synthetic macamides were evaluated in the THP-1 cell line. Preliminary biological evaluation indicated that most of these synthetic macamides did not present cytotoxicity (MTT assay) in the tested cell line with respect to the control (actinomycin D). Regarding the anti-inflammatory activity, several analogues had a greater potential for inhibition of TNF-α than natural macamides. Synthetic macamide 4a was the most active (IC₅₀ = 0.009 ± 0.001 μM) compared to the C87 (control). Through looking at the link between the chemical structure and the activity, our study pro

SUBMITTER: Tena Perez V 

PROVIDER: S-EPMC7652002 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature