256642-33-8Relevant academic research and scientific papers
Design and synthesis of azaisoflavone analogs as phytoestrogen mimetics
Gim, Hyo Jin,Li, Hua,Jung, So Ra,Park, Yong Joo,Ryu, Jae-Ha,Chung, Kyu Hyuck,Jeon, Raok
, p. 107 - 118 (2014/08/18)
A series of azaisoflavone analogs were designed and synthesized and their transactivation activities and binding affinities for ERα and ERβ were investigated. Among these compounds, 2b and 3a were the most potent with 6.5 and 1.1 μM of EC50, respectively. Molecular modeling study showed putative binding modes of the compound 3a in the active site of ERα and ERβ, which were similar with that of genistein and provided insight of the effect of N-alkyl substitution of azaisoflavones on ERβ activity. Also, a biphasic effect of azaisoflavone analogs on MCF-7 cell growth depending on their concentrations was investigated.
Ru(ii)-catalyzed intermolecular ortho-C-H amidation of aromatic ketones with sulfonyl azides
Bhanuchandra,Ramu Yadav,Rit, Raja K.,Rao Kuram, Malleswara,Sahoo, Akhila K.
supporting information, p. 5225 - 5227 (2013/06/27)
Ru(ii)-catalyzed intermolecular ortho-C-H amidation of weakly coordinating aromatic ketones with sulfonyl azides is reported. The developed reaction protocol can be extended to various substituted aromatic ketones to afford a wide range of desired C-N bond formation products in good yields.
Synthesis of azaisoflavones and their inhibitory activities of NO production in activated microglia
Jin, Guo Hua,Ha, Sang Keun,Park, Hye Min,Kang, Bomi,Kim, Sun Yeou,Kim, Hee-Do,Ryu, Jae-Ha,Jeon, Raok
supporting information; experimental part, p. 4092 - 4094 (2009/04/10)
A series of azaisoflavones were synthesized and their biological activities were evaluated for nitric oxide (NO) production and inducible NO synthase (iNOS) expression in BV-2 microglia cell lines. Among these compounds, compound 8d was the most potent with IC50 7.83 μM for inhibition of NO production. Also, compound 8d inhibited expression of iNOS in LPS-induced BV2 cells. This result suggests that compound 8d inhibited the production of NO by suppressing the expression of iNOS.
Acetylated dimethoxyaniline as a key intermediate for the synthesis of aminoflavones and quinolones
Deka, Nabajyoti,Hadjeri, Mohamed,Lawson, Martin,Beney, Chantal,Boumendjel, Ahcène
, p. 123 - 128 (2007/10/03)
3,5-Dimethoxyaniline was acetylated and found to be a key intermediate for the synthesis of a variety of biologically active aminoflavones and quinolones.
Synthesis and topoisomerase inhibitory activities of novel aza-analogues of flavones
Sui, Zhihua,Nguyen, Van N.,Altom, Jason,Fernandez, Jeffrey,Hilliard, Jamese J.,Bernstein, Jeffrey I.,Barrett, John F.,Ohemeng, Kwasi A
, p. 381 - 387 (2007/10/03)
A series of aza-flavones (3-hydroxy-2-phenyl-4-quinolones) were designed and synthesized as inhibitors of bacterial DNA-gyrase and mammalian topoisomerase II. Structure activity relationships of the compounds against each of the enzymes are discussed.
