Several quinolino-benzoxaborole derivatives have been prepared to start from aminobenzoxaboroles. These derivatives have been evaluated for their anti-cancer activity on human and murine cancer cell lines and based on...Several quinolino-benzoxaborole derivatives have been prepared to start from aminobenzoxaboroles. These derivatives have been evaluated for their anti-cancer activity on human and murine cancer cell lines and based on their relative non-toxicity, these compounds were further evaluated for their antibacterial activity against E. coli, B. subtilis, and M. smegmatis. The synthesized compounds were also evaluated for antifungal activity in C. albicans and C. neoformans.展开更多
Benzoxaborole,as a versatile scaffold,plays important roles in organic synthesis,molecular recognition and supramolecular chemistry.It is also a privileged structure in medicinal chemistry due to its desirable physico...Benzoxaborole,as a versatile scaffold,plays important roles in organic synthesis,molecular recognition and supramolecular chemistry.It is also a privileged structure in medicinal chemistry due to its desirable physicochemical and drug-like properties.Recently,benzoxaboroles were widely applied as antifungal,antibacterial,antiviral,anti-parasite,and anti-inflammatory agents.This review covers the properties,synthetic methods and applications of benzoxaboroles in medicinal chemistry.展开更多
This work investigated the effect of glyco-regioisomerism of glycopolymers on their dynamic interaction with benzoxaborole-containing polymers. Two kinds of glycopolymers, P-1-Gal and P-6-Gal, i.e. galactoside pendant...This work investigated the effect of glyco-regioisomerism of glycopolymers on their dynamic interaction with benzoxaborole-containing polymers. Two kinds of glycopolymers, P-1-Gal and P-6-Gal, i.e. galactoside pendant group linked to the identical main chain through its anomeric(C1) and C6-hydroxyl group position, respectively, were studied. We found that P-6-Gal showed stronger binding strength to the PNIPAM-co-PBOB polymer than P-1-Gal did, which controlled the macroscopic property of the resultant hydrogels at a molecular level.展开更多
A novel pyrrolo-benzoxaborole,6-（pyrrol-1-yl）-1,3-dihydro-1-hydroxy-2,1-benzoxaborole,was synthesized with 27%overall yield over six steps from 2-bromo-1-methyl-4-nitrobenzene as starting material.Its derivatization...A novel pyrrolo-benzoxaborole,6-（pyrrol-1-yl）-1,3-dihydro-1-hydroxy-2,1-benzoxaborole,was synthesized with 27%overall yield over six steps from 2-bromo-1-methyl-4-nitrobenzene as starting material.Its derivatization was achieved via Friedel-Crafts reaction catalyzed by anhydrous stannic chloride with various acyl chlorides giving 3-acyl-1-phenylpyrroles as the main products.展开更多
文摘Several quinolino-benzoxaborole derivatives have been prepared to start from aminobenzoxaboroles. These derivatives have been evaluated for their anti-cancer activity on human and murine cancer cell lines and based on their relative non-toxicity, these compounds were further evaluated for their antibacterial activity against E. coli, B. subtilis, and M. smegmatis. The synthesized compounds were also evaluated for antifungal activity in C. albicans and C. neoformans.
基金supported by National Natural Science Foundatoin of China(81222042)National Basic Research Program of China(2009CB918404,2012CB518001)
文摘Benzoxaborole,as a versatile scaffold,plays important roles in organic synthesis,molecular recognition and supramolecular chemistry.It is also a privileged structure in medicinal chemistry due to its desirable physicochemical and drug-like properties.Recently,benzoxaboroles were widely applied as antifungal,antibacterial,antiviral,anti-parasite,and anti-inflammatory agents.This review covers the properties,synthetic methods and applications of benzoxaboroles in medicinal chemistry.
基金supported by the National Natural Science Foundation of China (21604042, 21504016, 91527305)the Natural Science Foundation of Jiangsu Province of China (BK20150843)NUPTSF (NY215017, NY215080)
文摘This work investigated the effect of glyco-regioisomerism of glycopolymers on their dynamic interaction with benzoxaborole-containing polymers. Two kinds of glycopolymers, P-1-Gal and P-6-Gal, i.e. galactoside pendant group linked to the identical main chain through its anomeric(C1) and C6-hydroxyl group position, respectively, were studied. We found that P-6-Gal showed stronger binding strength to the PNIPAM-co-PBOB polymer than P-1-Gal did, which controlled the macroscopic property of the resultant hydrogels at a molecular level.
基金National Science Foundation of China(No.20702031)Ministry of Science and Technology of China (No.2009CB918404)E-Institutes of Shanghai Universities(EISU) Chemical Biology Division,and National Comprehensive Technology Platforms for Innovative Drug R&D(No.2009ZX09301-007) for financial support of this work
文摘A novel pyrrolo-benzoxaborole,6-（pyrrol-1-yl）-1,3-dihydro-1-hydroxy-2,1-benzoxaborole,was synthesized with 27%overall yield over six steps from 2-bromo-1-methyl-4-nitrobenzene as starting material.Its derivatization was achieved via Friedel-Crafts reaction catalyzed by anhydrous stannic chloride with various acyl chlorides giving 3-acyl-1-phenylpyrroles as the main products.
