A series of novel, azasugar-modified 2-monosubstituted, 2,6- and 2,7-bissubstituted anthraquinone derivatives have been synthesized by the nucleophilic substitution of N-alkylamino azasugar with mono-, bis（2-chloroac...A series of novel, azasugar-modified 2-monosubstituted, 2,6- and 2,7-bissubstituted anthraquinone derivatives have been synthesized by the nucleophilic substitution of N-alkylamino azasugar with mono-, bis（2-chloroacetamido）anthraquinones. Their cytotoxic activities against HeLa and MCF-7 ceils were preliminarily evaluated and compound 9a with mono-azasugar pendant at 2-position showed similar activity to the control drug （Cisplatin）.展开更多
Novel trimers of triphenylethylene-coumarin hybrid containing two amino side chains （5a-d and 6a-d） were designed and synthesized by the condensation of 1,3,5-benzenetricarboxylic acid with the varied amino monomeri...Novel trimers of triphenylethylene-coumarin hybrid containing two amino side chains （5a-d and 6a-d） were designed and synthesized by the condensation of 1,3,5-benzenetricarboxylic acid with the varied amino monomeric hybrids catalyzed by HATU and DIPEA at room temperature. The extended trimeric compound 6a （R = piperidinyl） exhibited significant anti-proliferative activity against three cancer cells at IC5o of near 10 μmol/L. UV-vis, fluorescence （lifetime） and thermal denaturation exhibited that 6a had significant interaction with Ct-DNA by the intercalative mode of binding. The order of their anti- proliferative activities was 6（a, d） 〉 5（a, d） and （5-6）a 〉 （5-6）d, respectively, in accordance with that of their DNA binding properties, which suggested that the prolonged linker （six carbons） and piperidinyl ~roun on the side chains are beneficial to DNA binding and the anti-tumor activity.展开更多
A series of novel naphthalimide derivatives modified by amino acids and their dichloroacetamide derivatives at the 3-position have been synthesized. Their cytotoxic activities were preliminarily evaluated against He/a...A series of novel naphthalimide derivatives modified by amino acids and their dichloroacetamide derivatives at the 3-position have been synthesized. Their cytotoxic activities were preliminarily evaluated against He/a, A549 and K562 cells, which showed that the length of the side chains of the amino acids influenced the cytotoxic activities. Moreover, compound 7d showed a very good cytotoxic activity against A549 cells with an IC50 value of 4.78 μmol L-1, Furthermore, the UV-vis, fluorescence, and circular dichroism （CD） spectroscopies and thermal denaturation experiment indicated that compounds 6a, 6d and 7a, 7d, as DNA intercalators, exhibited binding affinities with calf-thymus DNA （Ct-DNA）.展开更多
A novel triazatruxene-based fluorescent glycocluster was synthesized and its selective binding interactions with PNA lectin were investigated by fluorescence spectroscopy,CD spectroscopy,and a turbidity assay.The glyc...A novel triazatruxene-based fluorescent glycocluster was synthesized and its selective binding interactions with PNA lectin were investigated by fluorescence spectroscopy,CD spectroscopy,and a turbidity assay.The glycocluster exhibited a strong binding affinity for PNA lectin with a Stern-Volmer quenching constant of 5.8×10^5 mol^-1L展开更多
The management of acute ischemic stroke remains challenging due to its abrupt onset and the narrow treatment window,resulting in high rates of disability and mortality.Combination therapy for neuroprotection and neuro...The management of acute ischemic stroke remains challenging due to its abrupt onset and the narrow treatment window,resulting in high rates of disability and mortality.Combination therapy for neuroprotection and neurorepair strategies provided new hopes for subacute stroke treatment.Here we designed a multistage nanodelivery system that matches the unique microenvironment of the subacute phase of stroke,which utilizes calixarene as a building block to effectively load the neuroprotective drug simvastatin.The calixarene is designed with glycosidic linkages targeting the glucose transporter 1(GLUT1)on the blood-brain barrier(BBB)and azo bonds that are responsive to hypoxic conditions.Additionally,the decomposed calixarene molecules themselves possess intrinsic bio-activation to modulate inflammatory responses,achieving a multistage therapeutic approach that transitions from targeting to release and finally to treatment.This approach combines anti-inflammation and neuroprotection,providing a multi-level treatment strategy.This system was validated in a rat model of permanent middle cerebral artery occlusion(p MCAO),demonstrating that intravenous administration of the nanodelivery system repairs brain damage and improves motor function 24 h post-p MCAO induction.This work offers a precise and integrative strategy for stroke patients missing the acute therapy window to improve functional recovery and enhance the effect of comprehensive treatment.展开更多
基金supported by the National Natural Science Foundation of China(Nos.21372059 and 21172051)the Hebei Key Basic Research(No.12966417D)+1 种基金the Hebei Natural Science Foundation(No.B2012201041)the Foundation of Hebei Education Department(No.YQ2013006)
文摘A series of novel, azasugar-modified 2-monosubstituted, 2,6- and 2,7-bissubstituted anthraquinone derivatives have been synthesized by the nucleophilic substitution of N-alkylamino azasugar with mono-, bis（2-chloroacetamido）anthraquinones. Their cytotoxic activities against HeLa and MCF-7 ceils were preliminarily evaluated and compound 9a with mono-azasugar pendant at 2-position showed similar activity to the control drug （Cisplatin）.
基金the National Natural Science Foundation of China(NSFC,No.20902016)
文摘Novel trimers of triphenylethylene-coumarin hybrid containing two amino side chains （5a-d and 6a-d） were designed and synthesized by the condensation of 1,3,5-benzenetricarboxylic acid with the varied amino monomeric hybrids catalyzed by HATU and DIPEA at room temperature. The extended trimeric compound 6a （R = piperidinyl） exhibited significant anti-proliferative activity against three cancer cells at IC5o of near 10 μmol/L. UV-vis, fluorescence （lifetime） and thermal denaturation exhibited that 6a had significant interaction with Ct-DNA by the intercalative mode of binding. The order of their anti- proliferative activities was 6（a, d） 〉 5（a, d） and （5-6）a 〉 （5-6）d, respectively, in accordance with that of their DNA binding properties, which suggested that the prolonged linker （six carbons） and piperidinyl ~roun on the side chains are beneficial to DNA binding and the anti-tumor activity.
基金supported by the National Natural Science Foundation of China(Nos.21372059 and 21172051)the Hebei Natural Science Foundation(No.B2012201041)the Foundation of Hebei Education Department(No.YQ2013006)
文摘A series of novel naphthalimide derivatives modified by amino acids and their dichloroacetamide derivatives at the 3-position have been synthesized. Their cytotoxic activities were preliminarily evaluated against He/a, A549 and K562 cells, which showed that the length of the side chains of the amino acids influenced the cytotoxic activities. Moreover, compound 7d showed a very good cytotoxic activity against A549 cells with an IC50 value of 4.78 μmol L-1, Furthermore, the UV-vis, fluorescence, and circular dichroism （CD） spectroscopies and thermal denaturation experiment indicated that compounds 6a, 6d and 7a, 7d, as DNA intercalators, exhibited binding affinities with calf-thymus DNA （Ct-DNA）.
基金supported by the National Natural Science Foundation of China(Nos.21002020 and 21172051)the Hebei Natural Science Foundation(Nos.B2011201052 and B2012201041)
文摘A novel triazatruxene-based fluorescent glycocluster was synthesized and its selective binding interactions with PNA lectin were investigated by fluorescence spectroscopy,CD spectroscopy,and a turbidity assay.The glycocluster exhibited a strong binding affinity for PNA lectin with a Stern-Volmer quenching constant of 5.8×10^5 mol^-1L
基金supported by the National Natural Science Foundation of China(82241058,U20A20259)the Program of Tianjin Municipal Science and Technology(21JCZDJC00290)+4 种基金the Natural Science Foundation of Tianjin of China(22JCYBJC00980)the Fundamental Research Funds for the Central Universitiesthe Natural Science Foundation of Hebei Province(B2020201092,B2023201108,2567635H)the Foundation of Hebei Education Department(JZX2024018)the Advanced Talents Incubation Program of Hebei University(521100223250)。
文摘The management of acute ischemic stroke remains challenging due to its abrupt onset and the narrow treatment window,resulting in high rates of disability and mortality.Combination therapy for neuroprotection and neurorepair strategies provided new hopes for subacute stroke treatment.Here we designed a multistage nanodelivery system that matches the unique microenvironment of the subacute phase of stroke,which utilizes calixarene as a building block to effectively load the neuroprotective drug simvastatin.The calixarene is designed with glycosidic linkages targeting the glucose transporter 1(GLUT1)on the blood-brain barrier(BBB)and azo bonds that are responsive to hypoxic conditions.Additionally,the decomposed calixarene molecules themselves possess intrinsic bio-activation to modulate inflammatory responses,achieving a multistage therapeutic approach that transitions from targeting to release and finally to treatment.This approach combines anti-inflammation and neuroprotection,providing a multi-level treatment strategy.This system was validated in a rat model of permanent middle cerebral artery occlusion(p MCAO),demonstrating that intravenous administration of the nanodelivery system repairs brain damage and improves motor function 24 h post-p MCAO induction.This work offers a precise and integrative strategy for stroke patients missing the acute therapy window to improve functional recovery and enhance the effect of comprehensive treatment.
