899016-49-0Relevant academic research and scientific papers
Design, Synthesis, and Antiviral Activity of Novel Chalcone Derivatives Containing a Purine Moiety
Gan, Xiuhai,Wang, Yanjiao,Hu, Deyu,Song, Baoan
, p. 665 - 672 (2017/05/29)
To find new antiviral agents, novel chalcone derivatives containing a purine moiety were designed and synthesized by combining bioactive substructures. The antiviral activities of the derivatives against tobacco mosaic virus (TMV) and cucumber mosaic virus (CMV) were evaluated. Results showed that most of the derivatives showed antiviral activities. Compounds 3n and 3p exhibited excellent curative, protective and inactivation activities against TMV, with the EC50 values of 452.4, 416.2, 241.2 and 438.7, 418.6, 261.7 μg?mL?1, respectively, which were better than those of ribavirin (585.8, 436.0 and 268.7 μg?mL?1). Compounds 3n and 3p showed remarkable curative and protective activities against CMV. Compound 3n showed a moderate affinity to TMV coat protein, with binding constant Ka and Kd values of 1.5 × 104 L?mol?1 and 79.8 μmol?L?1, respectively. These findings provided an important structural insight for further designs of highly active chalcone derivatives and a basis for further study on their mechanism of action.
Evaluation and discovery of novel synthetic chalcone derivatives as anti-inflammatory agents
Wu, Jianzhang,Li, Jianling,Cai, Yuepiao,Pan, Yong,Ye, Faqing,Zhang, Yali,Zhao, Yunjie,Yang, Shulin,Li, Xiaokun,Liang, Guang
experimental part, p. 8110 - 8123 (2012/01/07)
Major anti-inflammatory agents, steroids and cyclooxygenase, were proved to have serious side effects. Here, a series of chalcone derivatives were synthesized and screened for anti-inflammatory activities. QSAR study revealed that the presence of electron-withdrawing groups in B-ring and electron-donating groups in A-ring of chalcones was important for inhibition of LPS-induced IL-6 expression. Further, compounds 22, 23, 26, 40, and 47 inhibited TNF-α and IL-6 release in a dose-dependent manner and decreased LPS-induced TNF-α, IL-1β, IL-6, IL-12, and COX-2 mRNA production. Mechanistically, compounds 23 and 26 interfered with JNK/NF-κB signaling and dose-dependently prevented ERK and p38 activation. In addition, 23 and 26 exhibited a significant protection against LPS-induced death and were able to block high glucose-activated cytokine profiles in macrophages. Together, these data show a series of anti-inflammatory chalcones with potential therapeutic effects in inflammatory diseases.
