- Synthesis of 3-Ferrocenyl Isocoumarins
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The derivatives of 3-ferrocenyl isocoumarin were synthesized by the condensation of substituted homothphalic anhydride with ferrocene using phosphoric acid or anhydrous aluminium chloride as cyclising agent. Substituted homophthalic acid did not condense with ferrocene so homophthalic acids were converted into their anhydride and then allowed to react with ferrocene in the presence of polyphosphoric acid or in the presence of anhydrous aluminium chloride using dichloromethane as the solvent to give 3-ferrocenyl isocoumarins. 7-Methoxy, 6-methyl, 5,7-dihydroxy, 6,7-dimethoxy and 5,7-dimethoxy derivatives of 3-ferrocenyl isocoumarin were synthesized. All the compounds were characterised by melting point determination, elemental and spectral analysis.
- Sinha, Neeta
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p. 976 - 979
(2020/11/25)
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- Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti-breast cancer agents
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The estrogen receptors have played important roles in breast cancer development and progression. Selective estrogen receptor modulators, such as Tamoxifen, have showed great benefits in the treatment and prevention of breast cancer. But the disadvantages of induction of endometrial cancer and drug resistance have limited their use. Multiple ligand which act at multiple biomolecular targets may exert favorable advantages of improved efficacy with lower incidence of side effects. In this work, we described the synthesis and evaluation of a series of 6-aryl-indenoisoquinolone derivatives as dual ERα and VEGFR-2 inhibitors. These compounds presented good ERα binding affinity and ERα antagonistic activity, as well as potent VEGFR-2 inhibitory potency. They also possessed excellent anti-proliferative activities against MCF-7, MDA-MB-231, Ishikawa and HUVEC cell lines. Further investigation of selective compound 21c showed that it was able to inhibit the activation of VEGFR-2 and the signaling transduction of Raf-1/MAPK/ERK pathway in MCF-7 cells.
- Tang, Zhichao,Wu, Chengzhe,Wang, Tianlin,Lao, Kejing,Wang, Yejun,Liu, Linyi,Muyaba, Moses,Xu, Pei,He, Conghui,Luo, Guoshun,Qian, Zhouyang,Niu, Shaoxiong,Wang, Lijun,Wang, Ying,Xiao, Hong,You, Qidong,Xiang, Hua
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p. 328 - 339
(2016/06/01)
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- 3-PHENYL-7-HYDROXY-ISOCOUMARINS AS MACROPHAGE MIGRATION INHIBITORY FACTOR (MIF) INHIBITORS
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This invention relates to 3-phenyl-7-hydroxy-isocoumarin compounds which are MIF inhibitors, compositions comprising said inhibitors and methods for treating or preventing diseases associated with MIF.
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Page/Page column 36
(2016/01/21)
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- Synthesis and biological evaluation of 2,3-diaryl isoquinolinone derivatives as anti-breast cancer agents targeting ERα and VEGFR-2
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The estrogen receptor α is recognized as important pharmaceutical target for breast cancer therapy, and vascular endothelial growth factor receptors (VEGFRs) play important roles in tumor angiogenesis including breast cancer. A series of 2,3-diaryl isoqui
- Tang, Zhichao,Niu, Shaoxiong,Liu, Fei,Lao, Kejing,Miao, Jingshan,Ji, Jinzi,Wang, Xiang,Yan, Ming,Zhang, Luyong,You, Qidong,Xiao, Hong,Xiang, Hua
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supporting information
p. 2129 - 2133
(2014/05/06)
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- ENANTIOSELECTIVE ORGANIC ANHYDRIDE REACTIONS
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Disclosed herein is enantioselective synthetic method comprising reacting an enolisable C4-C50 organic anhydride with a second compound selected from the group consisting of an aldehyde, a ketone, an aldimine, a ketimine or a Michael Acceptor in the presence of a bifunctional organocatalyst. The reaction may find particular utility in the enantioselective synthesis of medicinally relevant heterocycles, such as dihydroisocoumarins and dihydroisoquinolinones.
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Page/Page column
(2013/09/26)
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- Enantioselective organic anhydride reactions
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Disclosed herein is enantioselective synthetic method comprising reacting an enolisable C4-C50 organic anhydride with a second compound selected from the group consisting of an aldehyde, a ketone, an aldimine, a ketimine or a Michael Acceptor in the presence of a bifunctional organocatalyst. The reaction may find particular utility in the enantioselective synthesis of medicinally relevant heterocycles, such as dihydroisocoumarins and dihydroisoquinolinones.
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Paragraph 0074
(2013/09/26)
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- A catalytic asymmetric reaction involving enolizable anhydrides
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In the presence of a highly efficient novel bifunctional organocatalyst at low loadings under mild conditions, enolizable homophthalic anhydrides can be added to a range of aromatic and aliphatic aldehydes to give dihydroisocoumarins, with excellent yields and diastereo-and enantiocontrol (up to 99% ee).
- Cornaggia, Claudio,Manoni, Francesco,Torrente, Esther,Tallon, Sean,Connon, Stephen J.
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scheme or table
p. 1850 - 1853
(2012/06/16)
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- A short and efficient construction of the dibenzo[c,h]chromen-6-one skeleton
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We hereby report a major revision of the synthetic methodology for construction of the dibenzochromenone skeleton. Homophthalic acid derivatives were reacted with thionylchloride/DMF in the presence of NaN 3. As the main product, dibenzochromen
- Delioemeroglu, Murat K.,Oezcan, Sevil,Balcia, Metin
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scheme or table
p. 148 - 160
(2010/08/04)
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- Method for improving the efficiency of ruminant feed utilization
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Phthalides enhance propionate production and inhibit methane production in the rumen and are thus useful for improving feed utilization efficiency in ruminant animals.
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