24533-47-9Relevant academic research and scientific papers
Synthesis and cytotoxic evaluation of alkoxylated chalcones
Bai, Xiao-Guang,Xu, Chang-Liang,Zhao, Shuang-Shuang,He, Hong-Wei,Wang, Yu-Cheng,Wang, Ju-Xian
, p. 17256 - 17278 (2015/01/08)
A series of chalcones a1-20 bearing a 4-OMe groups on the A-ring were initially synthesized and their anticancer activities towards HepG2 cells evaluated. Subsequently, a series of chalcones b1-42 bearing methoxy groups at the 2′ and 6′-positions of the B-ring were synthesized and their anticancer activities towards five human cancer cell lines (HepG2, HeLa, MCF-7, A549 and SW1990) and two non-tumoral human cell lines evaluated. The results showed that six compounds (b6, b8, b11, b16, b18, b22, b23 and b29) displayed promising activities, with compounds b22 and b29 in particular showing higher levels of activity than etoposide against all five cancer cell lines. Compound b29 showed a promising SI value compared with both HMLE and L02 (2.1-6.5 fold in HMLE and > 33 > 103.1 fold in L02, respectively).
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.
Novel synthesis of 1,3,5-trisubstituted 2-pyrazolines promoted by chlorotrimethylsilane
Xie, Zengyang,Bian, Xiaoqin,Geng, Xin,Li, Shuangshuang,Wang, Cunde
, p. 52 - 54 (2008/09/19)
1,3,5-Trisubstituted-2-pyrazolines were effectively synthesised by utilising chlorotrimethylsilane as an efficient promoter in the cyclisation addition of Phenylhydrazine to chalcones under nitrogen in acetonitrile. The clean, mild reaction conditions, high yields and a simple workup of target compounds were attractive features of the reaction which enables a facile preparative procedure for building the pyrazoline ring.
