Background: This paper describes the synthesis of novel thiazolidin-4-one substituted pyrazole derivatives from the condensation reaction of hydrazide with acetophenone derivatives. Herein we describe the synthesis of fourteen compounds by microwave irradiation method. The synthesized compounds are in excellent yield by utilizing microwave irradiation heating. Objective: Compounds using different aromatic or heteroaromatic compounds should be synthesized and screened for their antibacterial activity to explore the possibility of pyrazole substituted thiazolidin- 4-ones as a novel series of antimicrobials. Method: Synthesis of thiazolidin-4-one substituted pyrazole derivatives was carried out under microwave radiation. Result: These compounds were identified on the basis of melting point range, Rf values, IR, 1HNMR and mass spectral analysis. These compounds were evaluated for their in vitro antimicrobial activity and their Minimum Inhibitory Concentration (MIC) was determined. Among them Comp. 4b and Comp. 4k possess appreciable antimicrobial and antifungal activities. Conclusion: A novel series of Thiazolidin-4-one substituted pyrazole were synthesized under microwave irradiation method and identified on the basis of melting point range, Rf values, IR, 1HNMR, mass spectral data and elemental analysis. The compounds were subjected to in vitro antimicrobial screening and their Minimum Inhibitory Concentrations (MIC) were determined. Among all the tested compounds, two compounds 4b and 4k exhibited moderate to significant activity against all the tested strains of bacteria and fungus were found to have appreciable antimicrobial activities. The results of antibacterial activity showed that compounds containing electron withdrawing groups were found to be more active than the compounds containing electron releasing groups.
A series of compounds, viz. 2‐(3‐(4‐aryl)‐1‐isonicotinoyl‐4,5‐dihydro‐1H‐pyrazol‐4‐yl)‐3‐phenylthiazolidin‐4‐one 4 (a–n), have been synthesized by reaction of 3 (a–n) with thioglycolic acid in the presence of zinc chloride. Compounds 3 (a–n) have been synthesized by amination of formylated pyrazoles 2 (A–B), which were synthesized by formylation of 1 (A–B) by Vilsmeier–Haack reagent (POCl3/DMF). Compounds 1 (A–B) were synthesized by condensation of hydrazide and substituted acetophenones under conventional method and microwave irradiation method. These compounds were identified on the basis of melting point range, Rf values, infrared, 1H NMR, and mass spectral analysis. These compounds were evaluated for their in vitro antimicrobial activity, and their minimum inhibitory concentration was determined. Among them, compound 4b and compound 4l possess appreciable antimicrobial and antifungal activities. Antibacterial activity results showed that compounds containing electron‐withdrawing groups were more active than compounds containing electron‐releasing groups.
Introduction Aurora-A kinase is associated with the Aurora kinase family which has been considered a striking anticancer target for the treatment of human cancers. Objective To design, synthesize, anticancer evaluation, and docking studies of novel 2-(1-isonicotinoyl-3-phenyl-1H-pyrazol-4-yl)-3-phenylthiazolidin-4-one derivatives as Aurora-A Kinase inhibitors. Method A total of 21 Pyrazole derivatives P (1–21) were synthesized by using the Vilsmeier Haack reagent which was characterized by FT-IR, 1H NMR, 13C NMR, and Mass spectroscopy. The synthesized derivatives were evaluated for their potential in vitro anticancer activity by MTT assay and Aurora-A kinase inhibition assay. Results The cytotoxicity assay (MTT assay) showed that compound P-6 exhibited potent cytotoxicity (IC50 = 0.37–0.44 μM) against two cancer (HCT 116 and MCF-7) cell lines, which were comparable to the standard compound, VX-680. Compound P-6 also showed inhibition of Aurora-A kinase with an IC50 value of 0.11 ± 0.03 µM. A Docking study was done to compound P-6 and P-20 into the active site of Aurora A kinase, in order to get the probable binding model for further study. Conclusion A series of 21 novel pyrazole derivatives P(1–21) were designed, synthesized, in vitro anticancer evaluation, and docking studies for Aurora A kinase inhibition. The results established that P-6 is a prospective aspirant for the development of anticancer agents targeting Aurora-A kinase.
Introduction Aurora-A kinase is associated with the Aurora kinase family which has been considered a striking anticancer target for the treatment of human cancers. Objective To design, synthesize, docking studies, and biological evaluation of novel 2-(1-isonicotinoyl-3-phenyl-1H-pyrazol-4-yl)-3-phenylthiazolidin-4-one derivatives as novel anticancer agents with Aurora-A Kinase inhibition.Method A total of 21 Pyrazole derivatives P (1-21) were synthesized by using the Vilsmeier Haack reagent which was characterized by FT-IR, 1H NMR, 13C NMR and Mass spectroscopy. The synthesized derivatives were evaluated for their potential in vitro anticancer activity and Aurora A kinase inhibitory activity.Results The cytotoxicity assay (MTT assay) showed that compound P-6 exhibited potent cytotoxicity (IC50 = 0.37- 0.44 μM) against two cancer (HCT 116 and MCF-7) cell lines, which were comparable to the standard compound, VX-680. Compound P-6 also showed inhibition of Aurora-A kinase with an IC50 value of 0.11±0.03 µM. A Docking study was done to compound P-6 and P-20 into the active site of Aurora A kinase, in order to get the probable binding model for further study. Conclusion A series of 21 novel pyrazole derivatives P(1-21) were designed, synthesized, docking studies, and evaluated for their in vitro anticancer activity by MTT assay and Aurora A kinase inhibitory activity. The results established that P-6 is a prospective aspirant for the development of anticancer agents targeting Aurora-A kinase.
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