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Synthesis and Trypanocidal Evaluation of Some Novel 2-(Substituted Benzylidene)-5, 7-Dibromo-6-Hydroxy-1-Benzofuran-3(2<i>H</i>)-Ones
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作者 K. L. Ameta Nitu S. Rathore +4 位作者 Biresh Kumar Edith S. Malaga M Manuela Verastegui P Robert H. Gilman B. L. Verma 《International Journal of Organic Chemistry》 2012年第3期295-301,共7页
Substituted 2-benzylidene-1-benzofuran-3-ones are commonly known as aurones. This class of bioactive heterocycles belongs to flavonoid family. The article intends to put forth the rational design and synthesis of a ne... Substituted 2-benzylidene-1-benzofuran-3-ones are commonly known as aurones. This class of bioactive heterocycles belongs to flavonoid family. The article intends to put forth the rational design and synthesis of a new series of aurones using 3’,5’-dibromo-2’,4’-dihydroxychalcones and copper bromide in presence of DMF-water mixture (8:2, v/v) for the first time. Preliminary bioassay shows that most of compounds have good trypanocidal activity against Trypanosoma cruzi at 10 μg/mL. Few compounds are equally potent to the standard drugs Benznidazole and Nifurtimox. The structures of the newly synthesized products 2a-n were established by elemental analysis, FTIR, 1H NMR, 13C NMR and mass spectroscopic studies. 展开更多
关键词 CHALCONES aurones TRYPANOSOMA CRUZI CHAGAS Disease Inhibition
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低端新兵——德国坦克AURON 5.1 Fun声卡
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作者 吉祥朵朵 《大众硬件》 2004年第5期66-66,共1页
低端产品虽然利润微薄,但出货量大,历来是兵家必争之地。Terra Tec(德国坦克)在成功进军中高端以后,适时推出其低端声卡AURON 5.1 Fun,做工扎实是其特点。
关键词 AURON 5.1 Fun声卡 音效芯片 输入输出接口 I/O接口
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Synthesis and Anti-VSMC Vegetation Activities of New Aurone Derivatives
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作者 FAN Rui BAN Shu-rong +2 位作者 FENG Xiu-e ZHAO Chen-xiao LI Qing-shan 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2012年第3期438-442,共5页
A series of new aurone derivatives was prepared by means of a practical route and their anti-vascular smooth muscle cells(VSMC) vegetation activities were evaluated by the 3-(4,5-dimethylthlazol-2-yl)-2,5- dipheny... A series of new aurone derivatives was prepared by means of a practical route and their anti-vascular smooth muscle cells(VSMC) vegetation activities were evaluated by the 3-(4,5-dimethylthlazol-2-yl)-2,5- diphenyltetrazolium bromide(MTT) method with tetrandrine as a positive contrast drug. The structures of the com- pounds were confirmed by 1H NMR, 13C NMR and electrospray ionization mass spectrometry(ESI-MS). Several new compounds exhibited promising activity against VSMC proliferation and the preliminary structure-activity relation- ships(SAR) were discussed in order to investigate the essential structures required for their bioactivities. 展开更多
关键词 Aurone derivative Anti-vascular smooth muscle cell(VSMC) vegetation activity SYNTHESIS
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Transforming the Snapdragon Aurone Biosynthetic Genes into Petunia Alters Coloration Patterns in Transgenic Flowers
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作者 Chen-Kuen Wang Yi-Chin Chin +2 位作者 Chih-Yu Lin Po-Yen Chen Kin-Ying To 《Advances in Bioscience and Biotechnology》 2015年第12期702-722,共21页
Aurones belong to a small class of flavonoids that provide yellow color in some floricultural plants including snapdragon. To explore novel flower coloration, two full-length cDNAs encoding chalcone 4'-O-glucosylt... Aurones belong to a small class of flavonoids that provide yellow color in some floricultural plants including snapdragon. To explore novel flower coloration, two full-length cDNAs encoding chalcone 4'-O-glucosyltransferase (designated as SRY4'CGT) and aureusidin synthase (designated as SRYAS1) in the aurone biosynthetic pathway were cloned from yellow flowers of snapdragon (Antirrhinum majus cv. Ribbon Yellow). Binary vectors were constructed and transformed separately into Petunia hybrida harboring blue flowers. Only a few flowers in 4 out of 9 transgenic SRY4'CGT plants showed variegated blue-white sectors;as time passed, amounts of variegated flowers and proportion of white sectors in the background blue color of the new-born flowers gradually increased, until finally, the petal color was completely white in all late-born flowers. In contrast, a few flowers in 3 out of 13 transgenic SRYAS1 plants showed variegated blue-white sectors;but, the amounts of variegated flowers did not increase over the whole flowering stage, and no complete white flowers were observed. RNA samples isolated from blue and white sectors of T1 transgenic SRY4'CGT plants were analyzed by reverse transcription-PCR, transgenic SRY4'CGT transcripts were detected in both sectors;however, transcripts of an upstream gene, chalcone synthase (CHS), were abundantly detected in the blue sectors but largely reduced in the white sectors, suggesting that the expression of CHS gene was suppressed in white sectors of transgenic plants. Furthermore, HPLC coupled with mass spectrometry demonstrated cyandin, malvidin and their derivatives were absent in white sectors, causing the white phenotype. Our findings may be attractive to molecular breeders. 展开更多
关键词 AGROBACTERIUM-MEDIATED Transformation AURONE Compound Identification Flower Color Genetic Engineering HPLC Profiling Suppression Transgene-Induced Gene Silencing
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Total synthesis of a hydrated aurone derivative
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作者 宋爱丽 王超 +1 位作者 吴艳芬 周立东 《Journal of Chinese Pharmaceutical Sciences》 CAS CSCD 2014年第10期688-693,共6页
The total synthesis of a hydrated aurone derivative, 2-benzyl-4-methoxy-2,6-dihydroxybenzofuran-3(2H)-one, has been achieved for the first time with 2.4% overall yield. Using phloroglucinol as the starting material,... The total synthesis of a hydrated aurone derivative, 2-benzyl-4-methoxy-2,6-dihydroxybenzofuran-3(2H)-one, has been achieved for the first time with 2.4% overall yield. Using phloroglucinol as the starting material, the key steps included Friedel-Crafts acylation, Williamson synthesis, hydrogenolysis, aldol condensation, enolization and Rubottom oxidation. 展开更多
关键词 Hydrated aurone Total synthesis Poplar gum
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Aurone derivatives as Vps34 inhibitors that modulate autophagy 被引量:3
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作者 Guodong Li Joshua William Boyle +6 位作者 Chung-Nga Ko Wu Zeng Vincent Kam Wai Wong Jian-Bo Wan Philip Wai Hong Chan Dik-Lung Ma Chung-Hang Leung 《Acta Pharmaceutica Sinica B》 SCIE CSCD 2019年第3期537-544,共8页
We report in this study the identification of a natural product-like antagonist(1a) of Vps34 as a potent autophagy modulator via structure-based virtual screening. Aurone derivative 1a strongly inhibited Vps34 activit... We report in this study the identification of a natural product-like antagonist(1a) of Vps34 as a potent autophagy modulator via structure-based virtual screening. Aurone derivative 1a strongly inhibited Vps34 activity in cell-free and cell-based assays. Significantly, 1a prevents autophagy in human cells induced either by starvation or by an mT OR inhibitor. In silico modeling and kinetic data revealed that 1a could function as an ATP-competitive inhibitor of Vps34. Moreover, it suppressed autophagy in vivo and without inducing heart or liver damage in mice. 1a could be utilized as a new motif for more selective and efficacious antagonists of Vps34 for the potential treatment of autophagy-related human diseases. 展开更多
关键词 AUTOPHAGY Natural products Vps34 Inhibitor STRUCTURE-BASED virtual screening VESICLE TRAFFICKING Heart or liver damage AURONE derivative
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Regioselective Synthesis of Aurone Derivatives via PBu_(3)-Catalyzed Cyclization of 2-Alkynoylphenols
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作者 Changqing Liu Zhannan Zhang +2 位作者 Jitan Zhang Xing Liu Meihua Xie 《Chinese Journal of Chemistry》 SCIE CAS CSCD 2014年第12期1233-1237,共5页
Aurone derivatives were synthesized in good to high yields by PBu_(3)-catalyzed intramolecular 5-exo cyclization of 2-alkynoylphenols.The reaction proceeds in high regioselectivity without forming 6-endo cyclization p... Aurone derivatives were synthesized in good to high yields by PBu_(3)-catalyzed intramolecular 5-exo cyclization of 2-alkynoylphenols.The reaction proceeds in high regioselectivity without forming 6-endo cyclization products. 展开更多
关键词 2-alkynoylphenol PBu_(3) intramolecular cyclization AURONE
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