Synthesis, biological evaluation and molecular docking studies of novel thiopyrimidine analogue as apoptotic agent with potential anticancer activity

Haffez, Hesham; Taha, Heba; Rabie, Maha A.; Awad, Samir M.; Zohny, Yasser M.

doi:10.1016/j.bioorg.2020.104249

Cited by 12 publications

(3 citation statements)

References 67 publications

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“…The antiproliferation and cytotoxicity were assessed using 3-(4,5-dimethylthiazol-2yl)-2,5-diphenyltetrazolium bromide (MTT, Serva) colorimetric assay [133]. To investigate the antiproliferation, all cell lines were seeded at a density of 20,000 cells per well in 96-well plates and allowed to adhere overnight.…”

Section: Antiproliferation Assay and Selectivity Index (Si) Calculationmentioning

confidence: 99%

Revealing the Potential Application of EC-Synthetic Retinoid Analogues in Anticancer Therapy

et al. 2021

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(1) Background and Aim: All-trans retinoic acid (ATRA) induces differentiation and inhibits growth of many cancer cells. However, resistance develops rapidly prompting the urgent need for new synthetic and potent derivatives. EC19 and EC23 are two synthetic retinoids with potent stem cell neuro-differentiation activity. Here, these compounds were screened for their in vitro antiproliferative and cytotoxic activity using an array of different cancer cell lines. (2) Methods: MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay, AV/PI (annexin V-fluorescein isothiocyanate (FITC)/propidium iodide (PI)), cell cycle analysis, immunocytochemistry, gene expression analysis, Western blotting, measurement of glutamate and total antioxidant concentrations were recruited. (3) Results: HepG2, Caco-2, and MCF-7 were the most sensitive cell lines; HepG2 (ATRA; 36.2, EC19; 42.2 and EC23; 0.74 µM), Caco-2 (ATRA; 58.0, EC19; 10.8 and EC23; 14.7 µM) and MCF-7 (ATRA; 99.0, EC19; 9.4 and EC23; 5.56 µM). Caco-2 cells were selected for further biochemical investigations. Isobologram analysis revealed the combined synergistic effects with 5-fluorouracil with substantial reduction in IC50. All retinoids induced apoptosis but EC19 had higher potency, with significant cell cycle arrest at subG0-G1, -S and G2/M phases, than ATRA and EC23. Moreover, EC19 reduced cellular metastasis in a transwell invasion assay due to overexpression of E-cadherin, retinoic acid-induced 2 (RAI2) and Werner (WRN) genes. (4) Conclusion: The present study suggests that EC-synthetic retinoids, particularly EC19, can be effective, alone or in combinations, for potential anticancer activity to colorectal cancer. Further in vivo studies are recommended to pave the way for clinical applications.

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Section: Antiproliferation Assay and Selectivity Index (Si) Calculationmentioning

confidence: 99%

Revealing the Potential Application of EC-Synthetic Retinoid Analogues in Anticancer Therapy

et al. 2021

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“…The steric hindrance of the compounds results in a negative effect on their anticancer activities. 31 On the observation of R 1 of the compounds, it was clear that the methyl and hydrogen substituted compounds showed better activity than chlorine substituted compounds. From the above perceptions, the order of the inhibitory activity of R substitution is H > CH 3 > CH 3 CH 2 > C 6 H 6 and that of R 1 substitution is H > CH 3 > Cl.…”

Section: Resultsmentioning

confidence: 98%

New N-(3′-acetyl-8-nitro-2,3-dihydro-1H,3′H-spiro[quinoline-4,2′-[1,3,4]thiadiazol]-5′-yl) acetamides induced cell death in MCF-7 cells via G2/M phase cell cycle arrest

et al. 2022

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“…Thiopyrimidine derivative (104) was synthesized and In-vitro screened for its potential use as anti-cancer agents, and showed significant and selective antiproliferative activity against MCF-7 cancer cell line with minimal cytotoxic effect [49].…”

Section: Figure 28 Pyrimidine Pyrazoline-anthracene Derivative (103) ...mentioning

confidence: 99%

An overview on synthesis and biological activity of pyrimidines

Mohamed¹,

Awad²,

El-tawab³

et al. 2022

World J. Adv. Res. Rev.

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Pyrimidines represent an important class of heterocycles containing two nitrogen atoms at position 1 and 3 of the six membered ring show wide range of biological activities. Numerous methods for the synthesis of pyrimidine and their diverse reactions offer enormous scope in the field of medicinal chemistry. Pyrimidine possesses wide spectrum of biological activities including antitubercular, antibacterial, antifungal, antiviral, anti-inflammatory, antimalarial, anticancer, and anti-HIV activity. The present review attempts to give brief information about the synthesis and various biological activities of pyrimidines and their derivatives.

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Synthesis, biological evaluation and molecular docking studies of novel thiopyrimidine analogue as apoptotic agent with potential anticancer activity

Cited by 12 publications

References 67 publications

Revealing the Potential Application of EC-Synthetic Retinoid Analogues in Anticancer Therapy

Revealing the Potential Application of EC-Synthetic Retinoid Analogues in Anticancer Therapy

New N-(3′-acetyl-8-nitro-2,3-dihydro-1H,3′H-spiro[quinoline-4,2′-[1,3,4]thiadiazol]-5′-yl) acetamides induced cell death in MCF-7 cells via G2/M phase cell cycle arrest

An overview on synthesis and biological activity of pyrimidines

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