An alternate method of synthesizing oligoglycerols from glycerolepichlorohydrinKOH mixtures at room temperature is proposed. This method involves using triethanolamine as a catalyst and produced a mixture of low molecular weight oligoglycerols, mainly di-and triglycerols. Second, the method was optimized for triglycerol yield, and the product obtained was found to be similar to the commercially available Triglycerol. Superior results were achieved using a combination of electrodialysis and ion-exchange as a purification step, which allowed for polyols synthesis with a total chlorine content below 120 ppm. To validate the applicability of oligoglycerol synthesized herein as a food, cosmetic, and pharmaceutical additive, preliminary toxicity studies including the cytotoxicity, comet, and micronucleus assays are discussed.
The pharmacological effects of carbon to silicon bioisosteric replacements have been widely explored in drug design and medicinal chemistry. Here, we present a systematic investigation of the impact of different silyl groups on the anticancer activity of mucobromic acid (MBA) bearing furan-2(5H)-one core. We describe a comprehensive characterization of obtained compounds with respect to their anticancer potency and selectivity towards cancer cells. All four novel compounds exert stronger antiproliferative activity than MBA. Moreover, 3b induce apoptosis in colon cancer cell lines. A detailed investigation of the mechanism of action revealed that 3b activity stems from the down-regulation of survivin and the activation of caspase-3. Furthermore, compound 3b attenuates the clonogenic potential of HCT-116 cells. Interestingly, we also found that depending on the type of the silyl group, compound selectivity towards cancer cells could be precisely controlled. Collectively, we demonstrated the utility of silyl groups for adjusting both the potency and selectivity of silicon-containing compounds. These data reveal a link between the types of silyl group and compound potency, which could have bearings for the design of novel silicon-based anticancer drugs.
1,8-Naphthalimides (benzo[de]isoquinoline-1,3-diones) modified in various positions of chromophore, provided an effective method for enhancing their anticancer activity and reducing undesirable toxic effects. To accomplish this goal, several new 6- and 6,7-substitued 1,8-naphthalimides containing a ω-hydroxylalkylamine side-chains of different length were obtained and evaluated in the report presented. Upon examination, it appeared that the replacement of the nitro groups in the chromophore slightly reduce its anticancer activities, whereas the presence of both nitro groups and ω-hydroxylalkylamine chain resulted in seriously increased anticancer activities. Obtained compounds showed Topo II inhibitory activity, moreover, influence of the substitution pattern on the ability to inhibit Topo II activity and cancer cells proliferation was observed.
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