Background: Cancer is a major cause of death all over the globe. Controlling cell division byinhibition of mitosis is the most successful clinical strategy for cancer treatment. The developmentof novel anticancer agents is the most important area in medicinal chemistry and drug discoveryresearch. Thiazolidine is the multifunctional nucleus which shows a number of pharmacologicalactivities like anticancer, anti-inflammatory, antioxidant, antibacterial, antifungal, antidiabetic,antihyperlipidemic and antiarthritic. Methods: In a present study series of 2-substituted-3-(1H-benzimidazole-2-yl)-thiazolidin-4-ones were designed, synthesized by the microwave-assisted system, and characterized bymelting point, IR, 1H NMR, and mass spectroscopy. All the newly synthesized compoundswere examined for their in vitro anticancer activity against breast cancer cell line MCF-7 bySulforhodamine B (SRB) assay. Results: The compounds AB-12 (GI50: 28.5 μg/ml) and AB-6 (GI50: 50.7 μg/ml) exhibitedsignificant cell growth inhibitory activity. Conclusion: These results indicate that compound AB-12 and AB-6 as related polo-like kinase1inhibitors compounds could be lead compounds for further development of anticanceragents.
In the present study we have selected antioxidants agents like Pioglitazone and Ascorbic acid were subjected for anti-cataract activity by in vitro glucose induced cataract model. In the procedure, goat lenses was incubated along with the aqueous humor solution containing 55mM glucose with Enalpril as a standard compound and Pioglitazone with varied concentration for the time interval of 72 hours at room temperature. There was a formation of blur layer on the goat eyeball occurs after 10-12 hours and this process complete after 72 hours. The cataract inducing lenses showing higher level of Na, MDA (P<0.001) along with the decreases in sodium-potassium ATPase activity and water-soluble protein content. The goat lenses treated with Ascorbic acid 40 µg/ml and Pioglitazone in concentrations of 15, 30, and 60 µg/ml showed increased protein content and prevent the formation of cataract.
Racecodotril (RCT), (N-[2-[(acetylthio) methyl]-1- oxo- 3- phenyl propyl] -glycine phenylmethyl ester) is an enkephalinase inhibitor. A rapid, specific, and economic UV spectrophotometric two methods have been developed using a solvent composed of methanol to determine the RCT content in bulk and pharmaceutical dosage formulations. Method A is the absorbance maxima method, in which λmax is 231 nm, linearity was observed in the concentration range 10 to 100 μg/mL for all the two methods, and exhibited good correlation coefficient for method A (r2 = 0.9991) and excellent mean recovery (98.22–102.77%). Method B is the area under curve (AUC), in which λmax 226 to 236 nm was selected for estimation of RCT and exhibited a good correlation coefficient for method B (r2 = 0.9953). The method was validated statistically and by recovery studies for linearity, precision, repeatability, and reproducibility. The obtained results reveal that the method can be employed for the routine analysis of RCT in bulks, as well as, in the commercial formulations.
Background: Cancer is a leading cause of death worldwide. Inhibiting mitosis is the most effective clinical technique for cancer treatment. The most critical field of medicinal chemistry and drug development research is the discovery of innovative anticancer drugs. Thiazolidine is a multifunctional nucleus with anticancer, anti-inflammatory, antioxidant, antibacterial, antifungal, antidiabetic, antihyperlipidemic, and antiarthritic properties. Methods: In this investigation, copper-nickel oxide nanoparticles synthesized by electrochemical synthesis yielded a significant yield. The capping was done with cetyltrimethyl ammonium bromide (CTAB), and the characterization was done with UV, FTIR, XRD, SEM-EDS, and TEM SAED. The biologically significant 2-(2-substituted-4-oxo-thiazolidine-3-yl)-1, 9-dihydro-purin-6-ones (GB-1 to GB-12) have been synthesized using copper-nickel oxide nanoparticles as a catalyst and by applying a microwave-assisted tool. It was characterized by melting point, IR, 1H NMR, 13C NMR and LC-HRMS/MS spectroscopy. Using Sulforhodamine B (SRB) test, all newly synthesized compounds were evaluated in vitro for anti-cancer, anti-inflammatory, antioxidant, and angiogenesis activities. Results: The compounds GB-6 (GI50: 30 μM), GB-8 (GI50: 10 μM) and GB-10 (GI50: 30 μM) exhibited significant cell growth inhibitory activity. The compounds GB-6, GB-8, GB-10 exhibited significant in vitro anti-inflammatory activity in the range of IC50:179.65-194.59 μg/ml as compared with aceclofenac (IC50:191.19μg/ml) and the antioxidant activity by DPPH radical scavenging assay the compounds GB-6 (IC50:11.96 µg/ml), GB-8 (IC50:10.67 µg/ml) and GB-10 (IC50: 9.08 µg/ml) exhibited excellent radical scavenging activities compared to ascorbic acid (IC50:13.04 µg/ml) and by the KMnO4 radical scavenging assay the compounds GB-2 (IC50:15.33 µg/ml), GB-4 (IC50:23.60 µg/ml), GB-8 (IC50:24.93 µg/ml), GB-10 (IC50:24.96 µg/ml) exhibited good radical scavenging activities compared to ascorbic acid (IC50: 26.55 µg/ml). The compounds GB-4, GB-8 and GB-10 at 10 nM test drug concentration and the GB-6 compounds at 100 nM test drug concentration show the maximum capillary growth inhibitory activity compared with thalidomide as a standard drug. Conclusion: Further development of anticancer drugs may be enabled by the discovery of related compounds to the anticancer agent, such as compound (GB-6), compound (GB-8), and compound (GB-10) as polo-like kinase 1 inhibitors.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.