60402-31-5Relevant academic research and scientific papers
Rapid synthesis of flavone-based monoamine oxidase (MAO) inhibitors targeting two active sites using click chemistry
Jia, Wei Zhen,Cheng, Feng,Zhang, Yin Jun,Ge, Jin Yan,Yao, Shao Q.,Zhu, Qing
, p. 141 - 151 (2016/12/16)
A new library of flavone derivatives targeting two active sites of monoamine oxidases (“aromatic cage” and substrate cavity) were designed and synthesized using click chemistry (CuAAC reaction) between 6-N3-2-phenyl chromones (Az1–Az2) and a series of alkynes (k1–k20). Their inhibitory activities against MAO isoforms (MAO-A and MAO-B) are evaluated. Compounds with fluorine, amide bonds, or amino bonds have shown better inhibition. The most potent flavone MAO inhibitor studied is Az2k19 (1.6?μm for MAO-A, 2.1?μm for MAO-B), while Az1k15 and Az2k15 displayed better selectivity toward MAO-B (SI?>?10). Docking studies are in accordance with our hypothesis that these inhibitors are most likely located at both the substrate cavity and the “aromatic cage”. Our results show that it is considerable to develop new MAO inhibitors from C6 substitution of flavone derivatives and that these compounds are also potential for the treatment of diseases associated with MAOs.
Investigation on the substitution effects of the flavonoids as potent anticancer agents: A structure-activity relationships study
Wang, Xiao-Bing,Yang, Lei,Kong, Ling-Yi,Liu, Wei,Guo, Qing-Long
, p. 1833 - 1849,17 (2020/07/30)
Three series of flavonoid analogues substituted with different aminomethyl substitutions at C-6, C-7, and C-8 were designed and synthesized for the structure-activity relationship studies as potent anticancer agents. The prepared analogues were evaluated for their in vitro inhibitory activity against the growth of the hepatic cancer cell lines HepG2 and SMMC-7721. Structure-activity relationships indicated that not only the compounds with amino methyl groups were more active than those without the groups in the same series but also the compounds substituted by aminomethyl groups at position C-8 were more active than those at positions C-6 and C-7.
6',2-(2'-Arylchromonyl) propionic acids, and analgesic and anti-inflammatory derivatives thereof
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, (2008/06/13)
Propionic acids and their functional derivatives having anti-inflammatory and analgesic properties correspond to the formula STR1 in which X is selected from phenyl, halophenyl, polyhalophenyl, lower alkylphenyl, trihalomethylphenyl, aryloxyphenyl, furyl and thienyl and R is selected from hydrogen, lower alkyl, lower omega-hydroxyalkyl, morpholinoethyl and lower dialkylaminoalkyl.
