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【期刊论文】Convenient and versatile synthesis of formyl-substituted benzoxaboroles
周虎臣, Long Ye†, Dazhong Ding, Yiqing Feng‡, Dongsheng Xie, Puhua Wu, Hui Guo, Qingqing Meng, Huchen Zhou*
Tetrahedron 65(2009)8738-8744,-0001,():
-1年11月30日
Despite of the medicinal significance of benzoxaboroles, with the newly discovered clinical compound AN2690 as an example, the synthetic method for rapid diversification of this novel scaffold is lacking. To this end, a versatile and scalable synthesis of formyl-substituted benzoxaboroles is described here. A key step is the mono-oxidation of the two hydroxyls in compound 4 by taking advantage of the stable oxaborole ring in non-coordinating solvents, which was devised based on the study of the intramolecular coordination and exchange properties.
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周虎臣, Tsutomu Akama *, Stephen J. Baker, Yong-Kang Zhang, Vincent Hernandez, Huchen Zhou, Virginia Sanders, Yvonne Freund, Richard Kimura, Kirk R. Maples, Jacob J. Plattner
Bioorganic & Medicinal Chemistry Letters 19(2009)2129-2132,-0001,():
-1年11月30日
A series of phenoxy benzoxaboroles were synthesized and screened for their inhibitory activity against PDE4 and cytokine release. 5-(4-Cyanophenoxy)-2,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2728) showed potent activity both in vitro and in vivo. This compound is now in clinical development for the topical treatment of psoriasis and being pursued for the topical treatment of atopic dermatitis.
Anti-inflammatory Phosphodiesterase Oxaborole Psoriasis Atopic dermatitis
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周虎臣, Stephen J. Baker, * Yong-Kang Zhang, Tsutomu Akama, Agnes Lau, Huchen Zhou, Vincent Hernandez, Weimin Mao, M. R. K. Alley, Virginia Sanders, and Jacob J. Plattner
Journal of Medicinal Chemistry, 2006, Vol. 49, No.15,-0001,():
-1年11月30日
A structure-activity relationship investigation for a more efficacious therapy to treat onychomycosis, a fungal infection of the toe and fingernails, led to the discovery of a boron-containing small molecule, 5-fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2690), which is currently in clinical trials for onychomycosis topical treatment.
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【期刊论文】Pattern Recognition of Proteins Based on an Array of Functionalized Porphyrins
周虎臣, Huchen Zhou, Laura Baldini, Jason Hong, Andrew J. Wilson, and Andrew D. Hamilton*
J. AM. CHEM. SOC. 2006, 128, 2421-2425,-0001,():
-1年11月30日
A practical protein-detecting array is desirable for its potential application in proteomics, medical diagnostics, and pathogen detection. Here, we report a novel protein-detecting array based on porphyrins containing peripheral amino acids as protein surface receptors. The array of porphyrin receptors showed a unique pattern of fluorescence change upon interaction with certain protein samples. Both metal and nonmetal-containing proteins and mixtures of proteins gave distinct patterns, allowing their unambiguous identification. The composite pattern for each sample was subjected to principal component analysis (PCA) to generate a clustering map for more practical visualization. Increasing the number of porphyrin receptors from eight to sixteen gave improved resolution, suggesting that this array is expandable to give satisfactory resolution for any given sample system by carefully maximizing the chemical diversity of the receptors.
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周虎臣, Huchen Zhou, a De-an Wang, b, c Laura Baldini, a Eileen Ennis, a Rishi Jain, a Adam Carie, c Sa¨ıd M. Sebti*b, c and Andrew D. Hamilton*a
Org. Biomol. Chem., 2006, 4, 2376-2386,-0001,():
-1年11月30日
Platelet-derived growth factor (PDGF) and its receptor PDGFR are required for tumor growth and angiogenesis, so disruption of the PDGF–PDGFR interaction should lead to starvation of tumors and reduction of tumor growth. Potent PDGF antagonists have been discovered through the synthesis of a series of calix[4]arene-based compounds that are designed to bind to the three-loop region of PDGF. The effect of lower-rim alkylation, linker and number of interacting head groups on the calix[4]arene scaffold on PDGF affinity and cellular activity has been investigated.
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