Four new polyhydroxylated steroids plaksterols A–D(1–4), together with two known related steroids ergost-7,9(11),22-trien-3β,5α,6α-triol(5) and ergosta-6β-methoxy-7,22-diene-3β,5α-diol(6), were isolated from m...Four new polyhydroxylated steroids plaksterols A–D(1–4), together with two known related steroids ergost-7,9(11),22-trien-3β,5α,6α-triol(5) and ergosta-6β-methoxy-7,22-diene-3β,5α-diol(6), were isolated from methanol extract of the South China Sea marine sponge Plakortis sp. Their structures were identified by spectroscopic analysis, including NMR, MS, and IR. The cytotoxicity of the polyhydroxylated steroids were evaluated, and compound 6 showed moderate inhibitory activities against K562, HL-60 and BEL-7402 cells.展开更多
A novel C-branched polyhydroxylated cyclic nitrone 25.which could be a valuable intermediate for the synthesis of C-branched pyrrolidine iminosugars,was synthesized starting from the commercially available i.-arabinos...A novel C-branched polyhydroxylated cyclic nitrone 25.which could be a valuable intermediate for the synthesis of C-branched pyrrolidine iminosugars,was synthesized starting from the commercially available i.-arabinose in 29.0%total yield.展开更多
Natural products have attracted the interest of the scientific community due to their importance and application.Alexine is a naturally polyhydroxylated pyrrolizidine alkaloid that is broadly found in plant sources an...Natural products have attracted the interest of the scientific community due to their importance and application.Alexine is a naturally polyhydroxylated pyrrolizidine alkaloid that is broadly found in plant sources and isolated from Alexa leiopetala.The biological properties such as glycosidase inhibitors,anti-virus,and anti-HIV activities,makes it interesting target for synthetical studies.This review reports different approaches and methodologies to the synthesis of alexine,and its stereoisomers as the target compounds in numerous studies.展开更多
The tittle compound has been synthesized successfully through the efficient andselective functional transformation of a-santonin. This procedure is the first successful approachdeveloped for synthesis of the dihydroag...The tittle compound has been synthesized successfully through the efficient andselective functional transformation of a-santonin. This procedure is the first successful approachdeveloped for synthesis of the dihydroagarofuran kind of sesquiterpenoids from the eduesmanolidesesquiterpenoid α-santonin.展开更多
Three pairs of novel 2-aryl-3,4,5-trihydroxypiperidines (6-8 and their enantiomers), the piperidine analogues of the pyrrolidine alkaloids radicamine A and radicamine B, were prepared from six- membered cyclic nitro...Three pairs of novel 2-aryl-3,4,5-trihydroxypiperidines (6-8 and their enantiomers), the piperidine analogues of the pyrrolidine alkaloids radicamine A and radicamine B, were prepared from six- membered cyclic nitrones through a concise two-step procedure, i.e., Grignard reagent addition and deprotection. These novel polyhydroxylated piperidine iminosugars were assayed against 10 types of enzymes. Only compound 8 exhibited weak inhibition (IC50 1080 μmol/L) against β-galactosidase from rat intestinal lactases.展开更多
1-epi-Castanospermine(5) was synthesized from readily available 2,3,4,6-tetra-O-benzyl-1-deoxynojirimycin(11) in 9 steps and 21% overall yield, with selective debenzylation, Barbier reaction and reductive aminatio...1-epi-Castanospermine(5) was synthesized from readily available 2,3,4,6-tetra-O-benzyl-1-deoxynojirimycin(11) in 9 steps and 21% overall yield, with selective debenzylation, Barbier reaction and reductive amination as the main reaction steps.展开更多
A series of C-7 modified analogues of casuarine have been synthesized from sugar-derived nitrone and assayed against various glycosidases. Introduction of C-7 aminomethyl or amide group led to sharp decrease of the in...A series of C-7 modified analogues of casuarine have been synthesized from sugar-derived nitrone and assayed against various glycosidases. Introduction of C-7 aminomethyl or amide group led to sharp decrease of the inhibitory activities.展开更多
基金supported by the National Key Research and Development Program of China (No. 2018YFC-0310903)the National Natural Science Foundation of China (Nos.21572210,41776136 and 81991522)NSFC-Shandong Joint Fund for Marine Science Research Centers (No. U1606403)。
文摘Four new polyhydroxylated steroids plaksterols A–D(1–4), together with two known related steroids ergost-7,9(11),22-trien-3β,5α,6α-triol(5) and ergosta-6β-methoxy-7,22-diene-3β,5α-diol(6), were isolated from methanol extract of the South China Sea marine sponge Plakortis sp. Their structures were identified by spectroscopic analysis, including NMR, MS, and IR. The cytotoxicity of the polyhydroxylated steroids were evaluated, and compound 6 showed moderate inhibitory activities against K562, HL-60 and BEL-7402 cells.
基金Financial support from National Basic Research Program of China(No.2012CB822101)the National Natural Science Foundation of China(No.21272240)+1 种基金National Science and Technology Major Projects for "Major New Drugs Innovation and Development"(No.2013ZX09508104)National Engineering Research Center for Carbohydrate Synthesis of Jiangxi Normal University
文摘A novel C-branched polyhydroxylated cyclic nitrone 25.which could be a valuable intermediate for the synthesis of C-branched pyrrolidine iminosugars,was synthesized starting from the commercially available i.-arabinose in 29.0%total yield.
文摘Natural products have attracted the interest of the scientific community due to their importance and application.Alexine is a naturally polyhydroxylated pyrrolizidine alkaloid that is broadly found in plant sources and isolated from Alexa leiopetala.The biological properties such as glycosidase inhibitors,anti-virus,and anti-HIV activities,makes it interesting target for synthetical studies.This review reports different approaches and methodologies to the synthesis of alexine,and its stereoisomers as the target compounds in numerous studies.
文摘The tittle compound has been synthesized successfully through the efficient andselective functional transformation of a-santonin. This procedure is the first successful approachdeveloped for synthesis of the dihydroagarofuran kind of sesquiterpenoids from the eduesmanolidesesquiterpenoid α-santonin.
基金Financial support from National Basic Research Program of China (Nos. 2012CB822101 and 2011CB808603)the Natural Science Foundation of China (Nos. 21272240 and 21102149)
文摘Three pairs of novel 2-aryl-3,4,5-trihydroxypiperidines (6-8 and their enantiomers), the piperidine analogues of the pyrrolidine alkaloids radicamine A and radicamine B, were prepared from six- membered cyclic nitrones through a concise two-step procedure, i.e., Grignard reagent addition and deprotection. These novel polyhydroxylated piperidine iminosugars were assayed against 10 types of enzymes. Only compound 8 exhibited weak inhibition (IC50 1080 μmol/L) against β-galactosidase from rat intestinal lactases.
基金Financial support from the National Natural Science Foundation of China(No.21272240)National Science and Technology Major Projects for“Major New Drugs Innovation and Development”(No.2013ZX09508104)National Engineering Research Center for Carbohydrate Synthesis of Jiangxi Normal University
文摘1-epi-Castanospermine(5) was synthesized from readily available 2,3,4,6-tetra-O-benzyl-1-deoxynojirimycin(11) in 9 steps and 21% overall yield, with selective debenzylation, Barbier reaction and reductive amination as the main reaction steps.
基金Financial support from the National Natural Science Foundation of China(Nos.21642012 and 21272240)National Science and Technology Major Projects for“Major New Drugs Innovation and Development”(No.2013ZX09508104)+1 种基金National Engineering Research Center for Carbohydrate Synthesis of Jiangxi Normal Universitysupported in part by a Grant-in-Aid for Scientific Research(C)(No.26460143)(AK)from the Japanese Society for the Promotion of Science(JSPS)
文摘A series of C-7 modified analogues of casuarine have been synthesized from sugar-derived nitrone and assayed against various glycosidases. Introduction of C-7 aminomethyl or amide group led to sharp decrease of the inhibitory activities.