14983-32-5

Upstream product

• 924-50-5 Methyl 3,3-dimethylacrylate 
• 98-80-6 phenylboronic acid 
• 638-10-8 ethyl 3-methylbut-2-enoate 
• 103-82-2 phenylacetic acid 
• 103-80-0 phenylacetyl chloride 
• 74143-89-8 5-phenyl-3,4-pentadien-2-one 
• 1364681-49-1 methyl 3-hydroxy-3-methyl-6-phenylhexa-4,5-dienoate 

Downstream Products

• 1434047-45-6 6-benzyl-4-methyl-2H-pyran-2-thione 
• 50405-58-8 6-benzyl-4-methyl-1-hydroxypyridin-2(1H)-one 

Relevant academic research and scientific papers

Development of Novel N-hydroxypyridone Derivatives as Potential Anti-Ischemic Stroke Agents

Our previous study had identified ciclopirox (CPX) as a promising lead compound for treatment of ischemic stroke. To find better neuroprotective agents, a series of N-hydroxypyridone derivatives based on CPX were designed, synthesized, and evaluated in this study. Among these derivatives, compound 11 exhibits significant neuroprotection against oxygen glucose deprivation and oxidative stress-induced injuries in neuronal cells. Moreover, compound 11 possesses good blood-brain barrier permeability and superior antioxidant capability. In addition, a complex of compound 11 with olamine-11·Ola possesses good water solubility, negligible hERG inhibition, and superior metabolic stability. The in vivo experiment demonstrates that 11·Ola significantly reduces brain infarction and alleviates neurological deficits in middle cerebral artery occlusion rats. Hence, compound 11·Ola is identified in our research as a prospective prototype in the innovation of stroke treatment.

Environmentally sustainable and chemo-selectively favorable synthesis of substituted 2H-Pyran-2-ones in water under MWI

In this paper, a novel synthesis of diversely substituted 2H-pyran-2-ones via the tandem reaction of 3-hydroxyhexa-4,5-allenic esters in water under the promotion of MWI has been developed. Compared with those reactions carried out in organic solvents, wa

Inhibition of cancer-associated mutant isocitrate dehydrogenases: Synthesis, structure-activity relationship, and selective antitumor activity

Mutations of isocitrate dehydrogenase 1 (IDH1) are frequently found in certain cancers such as glioma. Different from the wild-type (WT) IDH1, the mutant enzymes catalyze the reduction of α-ketoglutaric acid to d-2-hydroxyglutaric acid (D2HG), leading to cancer initiation. Several 1-hydroxypyridin-2-one compounds were identified to be inhibitors of IDH1(R132H). A total of 61 derivatives were synthesized, and their structure-activity relationships were investigated. Potent IDH1(R132H) inhibitors were identified with Ki values as low as 140 nM, while they possess weak or no activity against WT IDH1. Activities of selected compounds against IDH1(R132C) were found to be correlated with their inhibitory activities against IDH1(R132H), as well as cellular production of D2HG, with R2 of 0.83 and 0.73, respectively. Several inhibitors were found to be permeable through the blood-brain barrier in a cell-based model assay and exhibit potent and selective activity (EC50 = 0.26-1.8 μM) against glioma cells with the IDH1 R132H mutation.

Crystallographic investigation and selective inhibition of mutant isocitrate dehydrogenase

Mutations in isocitrate dehydrogenase (IDH), a key enzyme in the tricarboxylic acid cycle, have recently been found in ～75% glioma and ～20% acute myeloid leukemia. Different from the wild-type enzyme, mutant IDH1 catalyzes the reduction of α-ketoglutaric

Tandem reaction of 3-hydroxyhexa-4,5-allenic esters: A novel access to diversely substituted 2H-pyran-2-ones and indenes

A highly efficient synthesis of diversely substituted 2H-pyran-2-ones and indenes through Bronsted acid promoted tandem reaction of the readily obtainable 3-hydroxyhexa-4,5-allenic esters under extremely mild conditions has been developed. The Royal Society of Chemistry 2012.