Produção Nacional
Revisado por pares
Design and synthesis of pregnenolone/2-cyanoacryloyl conjugates with dual NF-κB inhibitory and anti-proliferative activities
2017; Elsevier BV; Volume: 27; Issue: 20 Linguagem: Inglês
10.1016/j.bmcl.2017.09.013
ISSN1464-3405
AutoresJiali Song, Juan Zhang, Changliang Liu, Chao Liu, Kongkai Zhu, Feifei Yang, Xigong Liu, João Paulo Figueiró Longo, Luís Alexandre Muehlmann, Ricardo Bentes Azevedo, Yuying Zhang, Yue‐Wei Guo, Cheng‐Shi Jiang, Hua Zhang,
Tópico(s)Genomics, phytochemicals, and oxidative stress
ResumoTwenty-five novel pregnenolone/2-cyanoacryloyl conjugates (6–30) were designed and prepared, with the aim of developing novel anticancer drugs with dual NF-κB inhibitory and anti-proliferative activities. Compounds 22 and 27–30 showed inhibition against TNF-α-induced NF-κB activation in luciferase assay, which was confirmed by Western blotting. Among them, compound 30 showed potent NF-κB inhibitory activity (IC50 = 2.5 μM) and anti-proliferative against MCF-7, A549, H157, and HL-60 cell lines (IC50 = 6.5–36.2 μM). The present study indicated that pregnenolone/2-cyanoacryloyl conjugate I can server as a novel scaffold for developing NF-κB inhibitors and anti-proliferative agents in cancer chemotherapy.
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