Synthesis of new morpholine - connected pyrazolidine derivatives and their antimicrobial, antioxidant, and cytotoxic activities

Kumar, Raghvendra; Moydeen, Meera; Al-Deyab, Salem S.; Manilal, Aseer; Idhayadhulla, Akbar

doi:10.1016/j.bmcl.2016.11.032

Cited by 32 publications

(15 citation statements)

References 15 publications

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“…The newly synthesized compounds (1a-1j) were screened for their cytotoxic activity according to the procedure suggested in previous literature [36].…”

Section: Cytotoxic Activitymentioning

confidence: 99%

Grindstone Chemistry: Design, One-Pot Synthesis, and Promising Anticancer Activity of Spiro[acridine-9,2′-indoline]-1,3,8-trione Derivatives against the MCF-7 Cancer Cell Line

et al. 2020

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In this study, the synthesis of one-pot 10-phenyl-3,4,6,7-tetrahydro-1H-spiro [acridine-9,2′-indoline]-1,3,8-trione derivatives was achieved via a four-component cyclocondensation reaction, which was carried out in solvent-free conditions, and using p-toluenesulfonic acid (p-TSA) as a catalyst. The product was confirmed by FT-IR, 1H-NMR, 13C-NMR, mass spectra, and elemental analysis. Furthermore, the anticancer activity was screened for all compounds. Among these compounds, compound 1c was more effective (GI50 0.01 µm) against MCF-7 cancer cell lines than standard and other compounds. Therefore, the objective of this study was achieved with a few promising molecules having been demonstrated to be potential anticancer agents.

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“…The newly synthesized compounds (1a-1j) were screened for their cytotoxic activity according to the procedure suggested in previous literature [36].…”

Section: Cytotoxic Activitymentioning

confidence: 99%

Grindstone Chemistry: Design, One-Pot Synthesis, and Promising Anticancer Activity of Spiro[acridine-9,2′-indoline]-1,3,8-trione Derivatives against the MCF-7 Cancer Cell Line

et al. 2020

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“…The newly synthesized compounds (2a–h), (3a–e), and (4a–e) were screened for their anticancer activity according to a previously published procedure (Surendra Kumar et al, 2017). Compounds (100 μM) were incubated in a microtiter plate with three different cell lines for 72 h, and cell viability was assessed by MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay.…”

Section: Methodsmentioning

confidence: 99%

Antimicrobial, anticoagulant, and cytotoxic evaluation of multidrug resistance of new 1,4-dihydropyridine derivatives

Ahamed

Arif

Mateen

et al. 2018

Saudi Journal of Biological Sciences

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A new series of 1,4-dihydropyridine derivatives ( and were systematically designed and synthesized via ultrasound irradiation methods with easy work-up and good yields. Compounds structures were confirmed by IR,H NMR, C NMR, and mass spectra. The synthesized compounds were screened for both antimicrobial and anticoagulant activities. Compound (MIC: 0.25 μg/mL) was highly active against and compound (MIC: 0.5 μg/mL) was also highly active against compared with ciprofloxacin. (MIC: 1 μg/mL) The antifungal activity of (MIC: 0.5 μg/mL) against was high relative to that of clotrimazole (MIC: 1 μg/mL). Anticoagulant activity was determined by activated partial thromboplastin time (APTT) and prothrombin time (PT) coagulation assays. Compound 4-(4-hydroxyphenyl)-2,6-dimethyl-,-bis(5-phenyl-1,3,4-thiadiazol-2-yl)-1,4-dihydropyridine-3,5-dicarboxamide (>1000 s in APTT assays) was highly active in anticoagulant screening compared with the reference of heparin. Cytotoxicity was evaluated using HepG2 (liver), HeLa (cervical), and MCF-7 (breast) cancer cell lines, with high toxicities observed for (GI = 0.02 μm) against HeLa cell line and (GI = 0.03 μm) equipotant against MCF-7 cell line. Therefore, the compounds and can serve as lead molecules for the development of new classes of antimicrobial and anticoagulant agent.

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“…The cytotoxic activity of the newly synthesized compounds (2a-2j) was tested using a previously described method ( Scudiere et al, 1988 ; Surendra Kumar et al, 2017 ). Compounds 2a-2j was tested in the MCF-7 cell line for 48 h using a single dose of primary anticancer assay at a concentration of 100 µm (MTT anticancer assay).…”

Section: Biological Screeningmentioning

confidence: 99%

New Chitosan Polymer Scaffold Schiff Bases as Potential Cytotoxic Activity: Synthesis, Molecular Docking, and Physiochemical Characterization

et al. 2022

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In this work, we synthesize the sulfonated Schiff bases of the chitosan derivatives 2a-2j without the use of a catalyst in two moderately straightforward steps with good yield within a short reaction time. The morphology and chemical structure of chitosan derivatives were investigated using FT-IR, NMR (1H—13C), XRD, and SEM. Furthermore, our chitosan derivatives were tested for their anticancer activity against the MCF-7 cancer cell line, and doxorubicin was used as a standard. In addition, the normal cell lines of the breast cancer cell MCF-10A, and of the lung cell MRC-5 were tested. Compound 2 h, with a GI50 value of 0.02 µM for MCF-7, is highly active compared with the standard doxorubicin and other compounds. The synthesized compounds 2a-2j exhibit low cytotoxicity, with IC50 > 100 μg/ml, against normal cell lines MCF-10A, MRC-5. We also provide the results of an in-silico study involving the Methoxsalen protein (1Z11). Compound 2h exhibits a higher binding affinity for 1Z11 protein (−5.9 kcal/mol) and a lower binding affinity for Doxorubicin (−5.3 kcal/mol) than certain other compounds. As a result of the aforementioned findings, the use of compound 2h has an anticancer drug will be researched in the future.

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Synthesis of new morpholine - connected pyrazolidine derivatives and their antimicrobial, antioxidant, and cytotoxic activities

Cited by 32 publications

References 15 publications

Grindstone Chemistry: Design, One-Pot Synthesis, and Promising Anticancer Activity of Spiro[acridine-9,2′-indoline]-1,3,8-trione Derivatives against the MCF-7 Cancer Cell Line

Grindstone Chemistry: Design, One-Pot Synthesis, and Promising Anticancer Activity of Spiro[acridine-9,2′-indoline]-1,3,8-trione Derivatives against the MCF-7 Cancer Cell Line

Antimicrobial, anticoagulant, and cytotoxic evaluation of multidrug resistance of new 1,4-dihydropyridine derivatives

New Chitosan Polymer Scaffold Schiff Bases as Potential Cytotoxic Activity: Synthesis, Molecular Docking, and Physiochemical Characterization

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