Eight novel 1,4-disubstituted phthalazines （7-14） were designed and synthesized. The structures of all the synthesized compounds were confirmed by IR,1H NMR, 13C NMR, MS and elemental analysis. Their in vitro cytoto...Eight novel 1,4-disubstituted phthalazines （7-14） were designed and synthesized. The structures of all the synthesized compounds were confirmed by IR,1H NMR, 13C NMR, MS and elemental analysis. Their in vitro cytotoxicity against cancer cell lines （Bel-7402 and HT- 1080） were evaluated by standard MTT assay. Among them, compounds 9 and 11 exhibited more potent cytotoxicity than cisplatin. 2007 Ping Gong. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.展开更多
A series of 1,4-substituted phthalazine derivatives were designed and synthesized.All the prepared compounds were screened for their cytotoxic activities against A549.HT-29 and MDA-MB-231 cell lines in vitro.Among the...A series of 1,4-substituted phthalazine derivatives were designed and synthesized.All the prepared compounds were screened for their cytotoxic activities against A549.HT-29 and MDA-MB-231 cell lines in vitro.Among them,compounds 7a-7h showed excellent selectivity for MDA-MB-231 cell line with IC50 values from 1 nmol/L to 0.92μmol/L.A preliminary SAR study of these derivatives was performed.展开更多
Studies show that two dimensional(2D)nanomaterial and its hybrid have a great promise in tribology for the special laminar microstructure.However,the majority of performed investigations about 2D graphitic carbon nitr...Studies show that two dimensional(2D)nanomaterial and its hybrid have a great promise in tribology for the special laminar microstructure.However,the majority of performed investigations about 2D graphitic carbon nitride(g-C_(3)N_(4))nanosheets are most focused on energy storage,catalysis,adsorption,rarely tribology.In the present study,g-C_(3)N_(4) supporting mono-dispersed Ag nanoparticle hybrid(g-C_(3)N_(4)/Ag)is prepared,and its microstructure and chemical composition are determined.More specifically,the tribological performance as the lubricating additive of poly phthalazinone ether sulfone ketone(PPESK)composite is investigated using the ball-on-disc friction tester.Moreover,the corresponding enhancement mechanism is well proposed based on the experimental analysis and theoretical simulation.Obtained results show that Ag nanoparticles with a size of about 10-20 nm are homogeneously anchored on g-C_(3)N_(4) nanosheets,favoring for good compatibility between g-C_(3)N_(4)/Ag and PPESK.It is found that when 0.3 wt%of g-C_(3)N_(4)/Ag is added to PPESK,the friction coefficient and wear rate of PPESK decrease by 68.9%and 97.1%,respectively.These reductions are mainly attributed to the synergistic self-lubricating effect of Ag nanoparticles and g-C_(3)N_(4) nanosheet,the formation of transfer film,as well as the limited effect of g-C_(3)N_(4)/Ag on the shear deformation of PPESK composite film.Furthermore,it is found that the proposed g-C_(3)N_(4)/Ag-PPESK composite still keeps reasonable friction-reducing and wear-resistant properties under heavy loads and high rotating speeds.The present study demonstrates that the proposed g-C_(3)N_(4)/Ag hybrid is an excellent lubricating additive for polymer composites.展开更多
Properties of dimethyl 3-（alkylamino）-5,10-dioxo-5,10-dihydro-1H-pyraolo[1,20b]phthalazine-1,2-dicarboxy-late and its derivatives were studied by means of ab initio method. NO2 derivative of title compound was synth...Properties of dimethyl 3-（alkylamino）-5,10-dioxo-5,10-dihydro-1H-pyraolo[1,20b]phthalazine-1,2-dicarboxy-late and its derivatives were studied by means of ab initio method. NO2 derivative of title compound was synthe- sized and the nature of its intramolecular hydrogen bond （HB） was investigated. Furthermore, the topological prop- erties of the electron density distributions for N--H＇＂O intramolecular bridges were analyzed in terms of the Bader theory of atoms in molecules （AIM）. The electron density （p） and Laplacian （V2p） properties, estimated by AIM calculations, indicated that O＇--H bond possesses low P and positive VZp values which are in agreement with elec- trostatic character of the HBs, whereas N--H bonds have covalent character （V2p〈0）. Moreover, steric effect of the t-Bu group on structure and topological parameters of pyrazolo[1,2-b]phthalazine conformers was studied. Fi- nally, the powerful method of Espinosa was used to obtain the H-bond energy.展开更多
文摘Eight novel 1,4-disubstituted phthalazines （7-14） were designed and synthesized. The structures of all the synthesized compounds were confirmed by IR,1H NMR, 13C NMR, MS and elemental analysis. Their in vitro cytotoxicity against cancer cell lines （Bel-7402 and HT- 1080） were evaluated by standard MTT assay. Among them, compounds 9 and 11 exhibited more potent cytotoxicity than cisplatin. 2007 Ping Gong. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.
文摘A series of 1,4-substituted phthalazine derivatives were designed and synthesized.All the prepared compounds were screened for their cytotoxic activities against A549.HT-29 and MDA-MB-231 cell lines in vitro.Among them,compounds 7a-7h showed excellent selectivity for MDA-MB-231 cell line with IC50 values from 1 nmol/L to 0.92μmol/L.A preliminary SAR study of these derivatives was performed.
基金This work was financially supported by the Project of Jiangsu Provincial Six Talent Peak(No.XCL-214)Foundation of State Key Laboratory of Solid lubrication(No.LSL-1709)Senior Intellectuals Fund of Jiangsu University(No.13JDG099).
文摘Studies show that two dimensional(2D)nanomaterial and its hybrid have a great promise in tribology for the special laminar microstructure.However,the majority of performed investigations about 2D graphitic carbon nitride(g-C_(3)N_(4))nanosheets are most focused on energy storage,catalysis,adsorption,rarely tribology.In the present study,g-C_(3)N_(4) supporting mono-dispersed Ag nanoparticle hybrid(g-C_(3)N_(4)/Ag)is prepared,and its microstructure and chemical composition are determined.More specifically,the tribological performance as the lubricating additive of poly phthalazinone ether sulfone ketone(PPESK)composite is investigated using the ball-on-disc friction tester.Moreover,the corresponding enhancement mechanism is well proposed based on the experimental analysis and theoretical simulation.Obtained results show that Ag nanoparticles with a size of about 10-20 nm are homogeneously anchored on g-C_(3)N_(4) nanosheets,favoring for good compatibility between g-C_(3)N_(4)/Ag and PPESK.It is found that when 0.3 wt%of g-C_(3)N_(4)/Ag is added to PPESK,the friction coefficient and wear rate of PPESK decrease by 68.9%and 97.1%,respectively.These reductions are mainly attributed to the synergistic self-lubricating effect of Ag nanoparticles and g-C_(3)N_(4) nanosheet,the formation of transfer film,as well as the limited effect of g-C_(3)N_(4)/Ag on the shear deformation of PPESK composite film.Furthermore,it is found that the proposed g-C_(3)N_(4)/Ag-PPESK composite still keeps reasonable friction-reducing and wear-resistant properties under heavy loads and high rotating speeds.The present study demonstrates that the proposed g-C_(3)N_(4)/Ag hybrid is an excellent lubricating additive for polymer composites.
文摘Properties of dimethyl 3-（alkylamino）-5,10-dioxo-5,10-dihydro-1H-pyraolo[1,20b]phthalazine-1,2-dicarboxy-late and its derivatives were studied by means of ab initio method. NO2 derivative of title compound was synthe- sized and the nature of its intramolecular hydrogen bond （HB） was investigated. Furthermore, the topological prop- erties of the electron density distributions for N--H＇＂O intramolecular bridges were analyzed in terms of the Bader theory of atoms in molecules （AIM）. The electron density （p） and Laplacian （V2p） properties, estimated by AIM calculations, indicated that O＇--H bond possesses low P and positive VZp values which are in agreement with elec- trostatic character of the HBs, whereas N--H bonds have covalent character （V2p〈0）. Moreover, steric effect of the t-Bu group on structure and topological parameters of pyrazolo[1,2-b]phthalazine conformers was studied. Fi- nally, the powerful method of Espinosa was used to obtain the H-bond energy.
