Development of the <b>β</b>-lactam type molecular scaffold for selective estrogen receptor <b>α</b> modulator action: synthesis and cytotoxic effects in MCF-7 breast cancer cells

Carr, Miriam; Knox, Andrew J. S.; Lloyd, David G.; Zisterer, Daniela M.; Meegan, Mary J.

doi:10.1080/14756366.2016.1210136

Cited by 4 publications

(3 citation statements)

References 64 publications

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“… a IC 50 values are half maximal inhibitory concentrations required to block the growth stimulation of cells. Values represent the mean for three experiments performed in triplicate; b The IC 50 value obtained for CA-4 (5.12 μM for MCF-7 and 26.41 μM for HCT-116) are in good agreement with reported values [ 39 , 40 ]. …”

Section: Figures Scheme and Tablesupporting

confidence: 84%

Synthesis, Anti-proliferative Activity, and Molecular Docking Study of New Series of 1,3-5-Triazine Schiff Base Derivatives

et al. 2020

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Based on the use of s-triazine as a scaffold, we report here a new series of s-triazine Schiff base derivatives and their anti-proliferative activity against two cancer cell lines: human breast carcinoma (MCF-7), and colon cancer (HCT-116) compared with tamoxifen as a reference compound. Several derivatives exhibited growth inhibition activity in the sub-micromolar range. The results reveal that the s-triazine Schiff base derivatives showed varied activities and that the substituents on the s-triazine core have a great effect on the anti-proliferative activity. Compounds with a piperidino and benzylamino substituent on the s-triazine moiety 4b and 4c were most effective in both cell lines compared to the reference compound used. In addition, compound 4b has a para chlorine atom on the benzylidine residue, demonstrating the most potent activity with IC50 values of 3.29 and 3.64 µM in MCF-7 and HCT-116, respectively. These results indicate that in general, the nature of the substituents on the triazine core and the type of substituent on the benzilyldene ring significantly influenced the anti-proliferative activity. The results obtained from the anti-proliferative activity and the molecular docking study indicate that s-triazine-hydrazone derivatives may be an excellent scaffold for the development of new anti-cancer agents.

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Section: Figures Scheme and Tablesupporting

confidence: 84%

Synthesis, Anti-proliferative Activity, and Molecular Docking Study of New Series of 1,3-5-Triazine Schiff Base Derivatives

et al. 2020

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“…After refluxing for 6 h, hot solution was filtered and the solvent evaporated under vacuum to obtain dry product 5 a-e. Schiff bases were used without any purification for final step. [42][43][44]…”

Section: General Procedures For the Preparation Of Nitrile Oxide Deri...mentioning

confidence: 99%

“…Compounds 2 a-b, 3 a-b, 4 a-b and 6 a-e have been synthesized, characterized and reported previously in literatures. [39][40][41][42][43][44] All of the used aniline derivatives and benzaldehyde derivatives are commercially available.…”

Section: Chemistrymentioning

confidence: 99%

Preparation of Novel 3,4,5‐Triaryl‐1,2,4‐Oxadiazole Derivatives: Molecular Docking and α‐Glucosidase assessment

Roustaei,

Saeedian Moghadam,

Faramarzi

et al. 2024

ChemistrySelect

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Diabetes mellitus (DM) has become a growing health problem, across all globe. Many factors have contributed into this issue, among them inappropriate lifestyle, unhealthy eating habits and growing spiritual/mental concerns are to be rated higher. Likewise much research needed to be diverted in progress for treatment of DM. Herein, we report synthesis and antidiabetic activity evaluation of ten novel phenolic derivatives of triaryl‐1,2,4‐oxadiazole 7 a–j. The compounds have synthesized using multistep reactions in acceptable purity and yields. Final step was done using 1,3‐dipolar cycloaddition reaction between various Schiff bases and arylnitrile oxides. 7 a–j were characterized by spectroscopic methods (1H NMR, 13C NMR, MS and IR) and their purities were confirmed using elemental analysis. All 7 a–j were evaluated for their α‐Glucosidase inhibitory activity. All compounds showed higher activity in inhibiting the enzyme, in comparison to standard, acarbose. Compounds 7 e and 7 g exerted the best activity with the IC50 value of 193.6 and 222.0 μM respectively. Furthermore, enzyme kinetic study approach was adopted to judge the effect of 7 e on enzyme inhibition. Finally, docking simulations revealed the possible mode of interactions between 7 e and 7 g and enzyme active sites. Final conclusion of results showed that oxadiazole scaffold/s are a potential antidiabetic target.

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Biacyl Substituted Monocycle β-LactamDerivative for Evaluation as Anticancer Agents

高¹

2019

WJCR

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Development of the β-lactam type molecular scaffold for selective estrogen receptor α modulator action: synthesis and cytotoxic effects in MCF-7 breast cancer cells

Abstract: The estrogen receptors (ERa and ERb) which are ligand inducible nuclear receptors are recognized as pharmaceutical targets for diseases such as osteoporosis and breast cancer.

Cited by 4 publications

References 64 publications

Synthesis, Anti-proliferative Activity, and Molecular Docking Study of New Series of 1,3-5-Triazine Schiff Base Derivatives

Synthesis, Anti-proliferative Activity, and Molecular Docking Study of New Series of 1,3-5-Triazine Schiff Base Derivatives

Preparation of Novel 3,4,5‐Triaryl‐1,2,4‐Oxadiazole Derivatives: Molecular Docking and α‐Glucosidase assessment

Biacyl Substituted Monocycle β-LactamDerivative for Evaluation as Anticancer Agents

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