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Practical and diastereospecific three-component 1,3-dipolar cycloaddition reactions of methyleneindolinones, isatins and diverse primary amino acids have been well established. A range of pyrrolidinyldispirooxindole scaffolds with wide structural diversity and complexity were obtained facilely in excellent yields under mild conditions, which hold promising applications in their further pharmacological studies. 相似文献
33.
Photoinitiated crosslinking of EPDM/inorganic filler blends and characterization of related properties 总被引:1,自引:0,他引:1
<正>Photoinitiated crosslinking of ethylene-propylene-diene terpolymer(EPDM) blends filled with calcium carbonate, talc and calcined kaolin(CK) in the presence of benzil dimethyl ketal as photoinitiator and trimethylolpropane triacrylate as crosslinker and their related properties have been studied by different analytical methods.The results from gel content and heat extension determination show that the efficiency of photocrosslinking of EPDM increases with increasing the content of diene and its molecular weight.The EPDM blends with 100 phr different inorganic fillers can be photocrosslinked to gel content of above 60%by 5 s UV-irradiation under optimum conditions.Under the same conditions of irradiation,the orders of photocrosslinking rate and final gel content are EPDM/CaCO_3EPDM/talcEPDM/CK.The data from thermogravimetric analysis,dynamic mechanical thermal analysis,electrical properties,mechanical tests and scanning electron microscopy show that UV irradiation crosslinking apparently enhances the thermal stability,mechanical properties and electrical properties of the photocrosslinked EPDM/inorganic filler samples.Although the attenuated total-reflection FTIR data show that inorganic fillers can promote the surface photo-oxidation of EPDM/inorganic filler samples with increasing the irradiation time,the above related properties of the photocrosslinked EPDM blends irradiated within 5 s are enough to satisfy many applications in the cable industry. 相似文献
34.
P. G. Morozov S. V. Kurbatov F. M. Dolgushin M. Yu. Antipin L. P. Olekhnovich 《Russian Chemical Bulletin》2004,53(9):2071-2074
The reactions of 2-(2-aminophenyl)benzimidazole with substituted isatins afforded the corresponding 5,6-dihydrospiro(benz[4,5]imidazo[1,2-c]quinazoline-6,3indolin)-2-ones. The spirocyclic structure of the reaction products was established by NMR spectroscopy and X ray diffraction analysis.Results of the study were presented at the International Conference Modern Trends in Organoelement and Polymer Chemistry dedicated to the 50th anniversary of the A. N. Nesmeyanov Institute of Organoelement Compounds of the Russian Academy of Sciences (May 30–June 4, 2004, Moscow).Published in Russian in Izvestiya Akademii Nauk. Seriya Khimicheskaya, No. 9, pp. 1987–1989, September, 2004. 相似文献
35.
The product from the reduction of ethyl spiro-3,3-(ethylenedioxy)-2-oxindole carboxylates (1) using borohydride salts has been found to be dependant upon both solvent and metal ion. With polar solvents and lithium bromide/sodium borohydride, spiro-3,3-(ethylenedioxy)-2-hydroxyindole carboxylates (2) are obtained in high yields whilst [2-(2-hydroxymethyl-[1,3]dioxolan-2-yl)-phenyl]-carbamic acid ethyl esters (3) are obtained using sodium borohydride in less polar solvents. 相似文献
36.
The addition of dimethyl acetylenedicarboxylate to isatin derivatives in the presence of triphenylphosphine leading to new highly functionalized γ-spirolactones is reported. 相似文献
37.
Nasima Arshad Muhammad Ismail Mir Fouzia Perveen Aneela Javed Memona Javaid Aamer Saeed Pervaiz Ali Channar Shahid Iqbal Farooqi Saad Alkahtani Jamshed Anwar 《Molecules (Basel, Switzerland)》2022,27(2)
Imidazolidine and thiazolidine-based isatin derivatives (IST-01–04) were synthesized, characterized, and tested for their interactions with ds-DNA. Theoretical and experimental findings showed good compatibility and indicated compound–DNA binding by mixed mode of interactions. The evaluated binding parameters, i.e., binding constant (Kb), free energy change (ΔG), and binding site sizes (n), inferred comparatively greater and more spontaneous binding interactions of IST-02 and then IST-04 with the DNA, among all compounds tested under physiological pH and temperature (7.4, 37 °C). The cytotoxic activity of all compounds was assessed against HeLa (cervical carcinoma), MCF-7 (breast carcinoma), and HuH-7 (liver carcinoma), as well as normal HEK-293 (human embryonic kidney) cell lines. Among all compounds, IST-02 and 04 were found to be cytotoxic against HuH-7 cell lines with percentage cell toxicity of 75% and 66%, respectively, at 500 ng/µL dosage. Moreover, HEK-293 cells exhibit tolerance to the increasing drug concentration, suggesting these two compounds are less cytotoxic against normal cell lines compared to cancer cell lines. Hence, both DNA binding and cytotoxicity studies proved imidazolidine (IST-02) and thiazolidine (IST-04)-based isatin derivatives as potent anticancer drug candidates among which imidazolidine (IST-02) is comparatively the more promising. 相似文献
38.
Andressa Oliveira Stefany Moura Luiz Pimentel Joo Neto Rafael Dantas Floriano Silva-Jr Monica Bastos Nubia Boechat 《Molecules (Basel, Switzerland)》2022,27(3)
Tyrosine kinase enzymes are among the primary molecular targets for the treatment of some human neoplasms, such as those in lung cancer and chronic myeloid leukemia. Mutations in the enzyme domain can cause resistance and new inhibitors capable of circumventing these mutations are highly desired. The objective of this work was to synthesize and evaluate the antiproliferative ability of ten new analogs that contain isatins and the phenylamino-pyrimidine pyridine (PAPP) skeleton, the main pharmacophore group of imatinib. The 1,2,3-triazole core was used as a spacer in the derivatives through a click chemistry reaction and gave good yields. All the analogs were tested against A549 and K562 cells, lung cancer and chronic myeloid leukemia (CML) cell lines, respectively. In A549 cells, the 3,3-difluorinated compound (3a), the 5-chloro-3,3-difluorinated compound (3c) and the 5-bromo-3,3-difluorinated compound (3d) showed IC50 values of 7.2, 6.4, and 7.3 μM, respectively, and were all more potent than imatinib (IC50 of 65.4 μM). In K562 cells, the 3,3-difluoro-5-methylated compound (3b) decreased cell viability to 57.5% and, at 10 µM, showed an IC50 value of 35.8 μM (imatinib, IC50 = 0.08 μM). The results suggest that 3a, 3c, and 3d can be used as prototypes for the development of more potent and selective derivatives against lung cancer. 相似文献
39.
Enantioselective Alkylation of N‐Arylhydrazones Derived from α‐Keto Esters and Isatin Derivatives through Asymmetric Phase‐Transfer Catalysis
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Dr. Qi‐Kai Kang Dr. Sermadurai Selvakumar Prof. Dr. Natarajan Arumugam Prof. Dr. Abdulrahman I. Almansour Prof. Dr. Raju Suresh Kumar Prof. Dr. Keiji Maruoka 《化学:亚洲杂志》2018,13(14):1780-1783
The phase‐transfer‐catalyzed asymmetric alkylation reactions of N‐arylhydrazones derived from α‐keto‐esters and isatin derivatives afford enantioenriched azo compounds that bear a tetra‐substituted carbon stereocenter in good yields with high chemo‐ and enantioselectivity. The alkylation products can be readily converted into chiral amino esters, hydrazine derivatives, and aza‐β‐lactams without loss of enantiopurity. 相似文献
40.