A series of 2-aziridinyl- and 2,3-bis(aziridinyl)-1,4-naphthoquinonyl sulfonate and acylate derivatives has been synthesized and evaluated for antimalarial activity in vitro against the human malaria parasite, Plasmodium falciparum (Vietnam Smith strain, chloroquine-resistant at the R3 level). The most active compounds, 2-aziridinyl-1,4-naphthoquinon-5-yl p-ethylbenzenesulfonate (13), 2-aziridinyl-1,4-naphthoquinon-5-yl p-tert-butylbenzenesulfonate (48), and 2-aziridinyl-5-hydroxy-1,4-naphthoquinone (5) produced 50% inhibition of the growth of P. falciparum at 9.6 x 10(-8), 2.4 x 10(-8), and 8.8 x 10(-8) M, respectively.
Three-dimensional (3D) printing has been playing an important role in diverse areas in medicine. In order to promote the development of tissue engineering, this study attempts to fabricate tissue engineering scaffolds using the inkjet printing technology. Sodium alginate, exhibiting similar properties to the native human extracellular matrix (ECM), was used as bioink. The jetted fluid of sodium alginate would be gelatinized when printed into the calcium chloride solution. The characteristics of the 3D-printed sodium alginate scaffold were systematically measured and analyzed. The results show that, the pore size, porosity and degradation property of these scaffolds could be well controlled. This study indicates the capability of 3D bioprinting technology for preparing tissue engineering scaffolds.
The solid N‐methyl‐2‐mono(substituted phenyl)benzothiazolines (1) are stable and can be stored in atmosphere, whereas they present different behavior in different solvents. They are relatively stable in alcohol and DMSO‐H2O. However, in other organic solvents such as acetone, CH2Cl2, CHCl3, EtOAc etc., the oxidation‐coupling reactions occurred spontaneously to give the corresponding disulfide dimers 2. The substituents at 2‐phenyl rings, reaction temperature and the acidities of the solutions exerted obvious impacts on the reaction rates and yields of 2. 12 samples of N‐methyl‐2‐(substituted phenyl)benzothiazolines (1) and 11 dimers 2 were evaluated in vitro vascular endothelial growth factor (VEGF) inhibitory activity in human breast cancer cell MDA‐MB‐231 with 2‐methoxyestradiol (2‐ME) as the positive reference and most of them showed potent VEGF inhibitory activity with the EC50 values of sub‐millimolar range. Among them, the compounds 1l, 1i, and 2d showed potent VEGF inhibitory activities and selectivities with EC50 values of 0.07, <0.12, and 0.03 mmol/L and SI values of 25, >32 and >32, respectively, which were about 10 times of those of 2‐ME (EC50=0.49 mmol/L, SI=3.37). The results further demonstrated that the scaffolds of 1 and 2 were privileged and merited further investigation as VEGF inhibitors.
The solid N-methyl-2-mono(substituted phenyl)benzothiazolines (1) are stable and can be stored in atmosphere, whereas they present different behavior in different solvents. They are relatively stable in alcohol and DMSO-H 2 O. However, in other organic solvents such as acetone, CH 2 Cl 2 , CHCl 3 , EtOAc etc., the oxidation-coupling reactions occurred spontaneously to give the corresponding disulfide dimers 2. The substituents at 2-phenyl rings, reaction temperature and the acidities of the solutions exerted obvious impacts on the reaction rates and yields of 2. 12 samples of N-methyl-2-(substituted phenyl)benzothiazolines (1) and 11 dimers 2 were evaluated in vitro vascular endothelial growth factor (VEGF) inhibitory activity in human breast cancer cell MDA-MB-231 with 2-methoxyestradiol (2-ME) as the positive reference and most of them showed potent VEGF inhibitory activity with the EC 50 values of sub-millimolar range. Among them, the compounds 1l, 1i, and 2d showed potent VEGF inhibitory activities and selectivities with EC 50 values of 0.07, <0.12, and 0.03 mmol/L and SI values of 25, >32 and >32, respectively, which were about 10 times of those of 2-ME (EC 50 =0.49 mmol/L, SI=3.37). The results further demonstrated that the scaffolds of 1 and 2 were privileged and merited further investigation as VEGF inhibitors.
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