179253-16-8Relevant articles and documents
Towards identifying potent new hits for glioblastoma
Sherer, Chris,Prabhu, Saurabh,Adams, David,Hayes, Joseph,Rowther, Farzana,Tolaymat, Ibrahim,Warr, Tracy,Snape, Timothy J.
, p. 1850 - 1861 (2018)
Glioblastoma is a devastating disease of the brain and is the most common malignant primary brain tumour in adults. The prognosis for patients is very poor with median time of survival after diagnosis measured in months, due in part to the tumours being highly aggressive and often resistant to chemotherapies. Alongside the ongoing research to identify key factors involved in tumour progression in glioblastoma, medicinal chemistry approaches must also be used in order to rapidly establish new and better treatments for brain tumour patients. Using a computational similarity search of the ZINC database, alongside traditional analogue design by medicinal chemistry intuition to improve the breadth of chemical space under consideration, six new hit compounds (14, 16, 18, 19, 20 and 22) were identified possessing low micromolar activity against both established cell lines (U87MG and U251MG) and patient-derived cell cultures (IN1472, IN1528 and IN1760). Each of these scaffolds provides a new platform for future development of a new therapy in this area, with particular promise shown against glioblastoma subtypes that are resistant to conventional chemotherapeutic agents.
Total synthesis and stereochemical revision of xiamenmycin A
Jiao, Xiaozhen,Yao, Yangyang,Yang, Beibei,Liu, Xiaoyu,Li, Xiaoyu,Yang, Hongguang,Li, Li,Xu, Jun,Xu, Minjuan,Xie, Ping
, p. 1805 - 1813 (2016)
The relative and absolute configurations of xiamenmycin A, a benzopyran compound isolated from Streptomyces xiamenensis 318 with a highly potent anti-fibrotic activity, have been characterized through the total synthesis. The key steps include the constru
SULFAMATE DERIVATIVE COMPOUNDS FOR USE IN TREATING OR ALLEVIATING PAIN
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, (2015/06/25)
The present invention relates to sulfamate derivative compounds and a composition for treating and/or alleviating pain containing the sulfamate derivative compounds or a pharmaceutically acceptable salt thereof as an active ingredient. More specifically,
Enantioselective copper-catalyzed intramolecular phenolic O-H bond insertion: Synthesis of chiral 2-carboxy dihydrobenzofurans, dihydrobenzopyrans, and tetrahydrobenzooxepines
Song, Xiao-Guang,Zhu, Shou-Fei,Xie, Xiu-Lan,Zhou, Qi-Lin
supporting information, p. 2555 - 2558 (2013/04/10)
Efficient: A copper-catalyzed enantioselective intramolecular insertion of carbenoids into phenolic O-H bonds has been developed. This method can be used for the synthesis of the title compounds in high yields and excellent enantioselectivities under mild and neutral conditions (see scheme). NaBAr F=sodium tetrakis[3,5-bis(trifluoromethyl)phenyl]borate. Copyright
Application of phenolate ion mediated intramolecular epoxide ring opening in the enantioselective synthesis of functionalized 2,3-dihydrobenzofurans and 1-benzopyrans
Dinda, Subal Kumar,Das, Sajal Kumar,Panda, Gautam
experimental part, p. 1886 - 1896 (2009/12/31)
The enantioselective synthesis of 2-isopropenyl-2,3-dihydrobenzofurans, 4-(2,3-dihydrobenzofuran-2-yl)-2-methylbut-3-en-2-ols, 2-hydroxymethyl chromans, and 4-chroman-2-yl-2-methylbut-3-en-2-ols has been achieved using Sharpless asymmetric epoxidation-der
β-Hydroxy-α-tosyloxy esters as chiral building blocks for the enantioselective synthesis of benzo-annulated oxa-heterocycles: scope and limitations
Das, Sajal Kumar,Panda, Gautam
, p. 4162 - 4173 (2008/09/19)
The enantioselective synthesis of benzo-annulated oxa-heterocycles 2,3-dihydrobenzofuran and 1-benzopyran derivatives is described using β-hydroxy-α-tosyloxy esters as chiral building blocks, which are easily accessible through the regioselective α-tosyla
A convergent approach to the mitomycin ring system
Coleman, Robert S.,Chen, Wei
, p. 1141 - 1144 (2007/10/03)
Matrix presented A novel stereoselective approach to the ring system of the mitomycins is described. The synthesis was based on a convergent strategy involving a stereocontrolled addition of a β-phenyl silyl enol ether to a pyrroline N-acyliminium ion followed by an intramolecular palladium-catalyzed aryl triflate amination to afford the (9R*,9aR*)-tetrahydropyrrolo[1,2-a]indole ring system.
ORTHO SUBSTITUTED AROMATIC COMPOUNDS USEFUL AS ANTAGONISTS OF THE PAIN ENHANCING EFFECTS OF E-TYPE PROSTAGLANDINS
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, (2008/06/13)
The invention relates to compounds of the formula (I): STR1 wherein A, B and D are various ring systems such as phenyl, R. sup.1 includes carboxy, R 3 is hydrogen or C 1-4 alkyl and Z is a linking group such as--(CH(R 5)) m--wherein m is 2, 3 or 4, and R 5 includes hydrogen and methyl; and pharmaceutically acceptable salts and in vivo hydrolysable esters or amides thereof, processes for preparing these compounds, pharmaceutical compositions comprising them, and their use in the treatment of pain.
