Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.

doi:10.1016/j.ejmech.2015.11.010

Paper

DOI: 10.1016/j.ejmech.2015.11.010

Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.

Published Jan 27, 2016 · F. Thaler, L. Moretti, Raffaella Amici

European journal of medicinal chemistry

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Abstract

Abstract hidden due to publisher request; this does not indicate any issues with the research. Click the full text link above to read the abstract and view the original source.

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Spirochromanes, with various cycloamines, show potential as potent HDAC inhibitors with good in vitro ADME profiles and molecular modeling insights.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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References

Citations

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Palladium-catalyzed stereoselective decarboxylative [4 + 2] cyclization of 2-methylidenetrimethylene carbonates with pyrrolidone-derived enones: Straightforward access to chiral tetrahydropyran-fused spiro-pyrrolidine-2,3-diones

Palladium-catalyzed asymmetric cycloaddition of 2-methylidenetrimethylene carbonate with pyrrolidone-derived enones produces functionalized tetrahydropyran-fused spirocyclic scaffolds with high yields and excellent en

2023·2citations·Ke Zhang et al.·Chinese Chemical Letters

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DOI: 10.1080/00397911.2023.2199360

An ultrasound assisted green protocol for the synthesis of quinoxaline based bisspirooxindoles: Crystal structure analysis, enone umpolung, DFT calculations, anti-cancer activity, and molecular docking studies

Ultrasound-assisted green synthesis of quinoxaline-based bisspirooxindoles yields novel compounds with promising anti-cancer activity, potentially serving as a lead for further development of novel anti-cancer agents.

2023·2citations·Sravanthi Baddepuri et al.·Synthetic Communications

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DOI: 10.4155/fmc-2021-0237

Design, synthesis and structure-activity relationship studies of novel spirochromanone hydrochloride analogs as anticancer agents.

Spirochromanone derivatives show promising anticancer activity, with the most potent compounds showing selective targeting of MCF-7 breast cancer cells and significant cytotoxicity.

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DOI: 10.1016/j.tet.2021.132297

Diastereoselective construction of structurally diverse trifluoromethyl bispiro-[oxindole-pyrrolidine-chromanone]s through [3+2] cycloaddition reactions

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2021·2citations·Zheng Li et al.·Tetrahedron

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DOI: 10.1016/j.bmc.2020.115813

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DOI: 10.2174/0929867325666180530094120

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2020·15citations·Faria Sultana et al.·Current medicinal chemistry

Current medicinal chemistry

DOI: 10.1016/J.CCLET.2019.03.029

Combined inhibition of HDAC and DNMT1 induces p85α/MEK-mediated cell cycle arrest by dual target inhibitor 208 in U937 cells

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2019·14citations·Yue Ren et al.·Chinese Chemical Letters

Chinese Chemical Letters

DOI: 10.1016/j.ejmech.2018.08.073

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2018·68citations·Rekha Sangwan et al.·European journal of medicinal chemistry

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Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.

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References

Citations

Palladium-catalyzed stereoselective decarboxylative [4 + 2] cyclization of 2-methylidenetrimethylene carbonates with pyrrolidone-derived enones: Straightforward access to chiral tetrahydropyran-fused spiro-pyrrolidine-2,3-diones

Palladium-catalyzed asymmetric cycloaddition of 2-methylidenetrimethylene carbonate with pyrrolidone-derived enones produces functionalized tetrahydropyran-fused spirocyclic scaffolds with high yields and excellent en

An ultrasound assisted green protocol for the synthesis of quinoxaline based bisspirooxindoles: Crystal structure analysis, enone umpolung, DFT calculations, anti-cancer activity, and molecular docking studies

Ultrasound-assisted green synthesis of quinoxaline-based bisspirooxindoles yields novel compounds with promising anti-cancer activity, potentially serving as a lead for further development of novel anti-cancer agents.

Design, synthesis and structure-activity relationship studies of novel spirochromanone hydrochloride analogs as anticancer agents.

Spirochromanone derivatives show promising anticancer activity, with the most potent compounds showing selective targeting of MCF-7 breast cancer cells and significant cytotoxicity.

Diastereoselective construction of structurally diverse trifluoromethyl bispiro-[oxindole-pyrrolidine-chromanone]s through [3+2] cycloaddition reactions

This study developed a straightforward and atom-economical method for preparing biologically important bispiro-[oxindole-pyrrolidine-chromanone]s with a CF3 motif, potentially valuable in medicinal chemistry.

A brief overview on recent advances in spiro[chromane-2,4'-piperidine]-4(3H)-one-functionalized compounds in medicinal chemistry research.

Recent advances in syntheses of spiro[chromane-2,4'-piperidine]-4(3H)-one-derived compounds show promise for developing new biologically active substances with potential utility in various fields.

Hydroxamic acid hybrids as the potential anticancer agents: An Overview.

Hydroxamic acid hybrids show potential as novel anticancer agents by overcoming drug resistance and improving specificity through rational design.

Zinc dependent Histone deacetylase inhibitors in cancer therapeutics: Recent update.

HDAC inhibitors show potential as a new class of targeted cancer therapeutics, offering insights into designing and synthesizing safe and selective compounds for molecular targeted therapy and combination drug therapy.

Combined inhibition of HDAC and DNMT1 induces p85α/MEK-mediated cell cycle arrest by dual target inhibitor 208 in U937 cells

A dual HDAC and DNMT inhibitor 208 induces G1 cell cycle arrest and apoptosis in U937 cells through the p85/MEK-mediated pathway, providing insights into potential mechanisms of multifunctional epigenetic inhibitors.

HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.

HDAC inhibitors show potential as a safe and effective anticancer therapeutic strategy, with potential for clinical application and synthesis of synthetic, hybrid, and natural classes.

Palladium-catalyzed stereoselective decarboxylative [4 + 2] cyclization of 2-methylidenetrimethylene carbonates with pyrrolidone-derived enones: Straightforward access to chiral tetrahydropyran-fused spiro-pyrrolidine-2,3-diones