586415-11-4Relevant academic research and scientific papers
Rapid access of some chloro-substituted isocoumarins and biological activity toward some pathogenic systems
Roy,Sarkar
, p. 2177 - 2181 (2005)
Sulphuric acid-catalyzed chloralhydrate condensation with different m-substituted benzoic acids formed trichlorophthalides 1, from which Zn + AcOH reduction afforded various dichloro derivatives 2. These derivatives 2 on treatment with alkaline Hg(OAc)su
Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti-breast cancer agents
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
, p. 328 - 339 (2016/06/01)
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.
3-PHENYL-7-HYDROXY-ISOCOUMARINS AS MACROPHAGE MIGRATION INHIBITORY FACTOR (MIF) INHIBITORS
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, (2016/01/21)
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.
Synthesis and biological evaluation of 2,3-diaryl isoquinolinone derivatives as anti-breast cancer agents targeting ERα and VEGFR-2
Tang, Zhichao,Niu, Shaoxiong,Liu, Fei,Lao, Kejing,Miao, Jingshan,Ji, Jinzi,Wang, Xiang,Yan, Ming,Zhang, Luyong,You, Qidong,Xiao, Hong,Xiang, Hua
, p. 2129 - 2133 (2014/05/06)
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
ENANTIOSELECTIVE ORGANIC ANHYDRIDE REACTIONS
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, (2013/09/26)
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.
Enantioselective organic anhydride reactions
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, (2013/09/26)
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.
A catalytic asymmetric reaction involving enolizable anhydrides
Cornaggia, Claudio,Manoni, Francesco,Torrente, Esther,Tallon, Sean,Connon, Stephen J.
, p. 1850 - 1853 (2012/06/16)
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).
Hydroxyl-Substituted sulfonylureas as potent inhibitors of specific [3H]Glyburide binding to rat brain synaptosomes
Hill, Ronald A.,Rudra, Sonali,Peng, Bo,Roane, David S.,Bounds, Jeffrey K.,Zhang, Yang,Adloo, Ahmad,Lu, Tiansheng
, p. 2099 - 2113 (2007/10/03)
We are seeking to discover potent CNS-active sulfonylureas with structural features that allow for the formation of several types of prodrugs. We report herein the syntheses of compounds comprising an initial series of hydroxyl-substituted analogues of the potent ATP-sensitive potassium channel blockers glyburide (glibenclamide) and gliquidone. Somewhat unexpectedly, several of the compounds were found to be comparably potent to glyburide as inhibitors of specific [3H]glyburide binding in rat brain preparations.
