Decarboxylative 1,3-dipolar cycloadditions of l-proline

RSC Advances, Journal Year: 2024, Volume and Issue: 14(12), P. 8481 - 8501

Published: Jan. 1, 2024

1,3-Dipolar cycloaddition is one of the important chemical reactions between a 1,3-dipole and dipolarophile to construct five-membered heterocyclic compound. As an available α-amino acid reactant, l-proline extensively used in 1,3-dipolar reactions. A diverse spectrum bioactive spiro fused N-heterocycles obtained through this synthetic approach. In review, we have described use synthesis various spiro- scaffolds.

Language: Английский

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Development of Novel Ecto-Nucleotide Pyrophosphatase/Phosphodiesterase 1 (ENPP1) Inhibitors for Tumor Immunotherapy

International Journal of Molecular Sciences, Journal Year: 2022, Volume and Issue: 23(13), P. 7104 - 7104

Published: June 26, 2022

The cyclic guanosine monophosphate-adenosine monophosphate synthase-stimulator of interferon genes-TANK-binding kinase 1-interferon regulating factor 3 (cGAS-STING-TBK1-IRF3) axis is now acknowledged as the major signaling pathway in innate immune responses. However, 2',3'-cGAMP a STING stimulator easily recognized and degraded by ecto-nucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1), which reduces effect tumor immunotherapy promotes metastatic progression. In this investigation, structure-based virtual screening strategy was adopted to discover eight candidate compounds containing zinc-binding quinazolin-4(3H)-one scaffold ENPP1 inhibitors. Subsequently, these novel inhibitors targeting were synthesized characterized NMR high-resolution mass spectra (HRMS). bioassays, 7-fluoro-2-(((5-methoxy-1H-imidazo[4,5-b]pyridin-2-yl)thio)methyl)quina-zolin-4(3H)-one(compound 4e) showed excellent activity against at molecular cellular levels, with IC50 values 0.188 μM 0.732 μM, respectively. Additionally, compound 4e had superior selectivity towards breast cancer cells (4T1) than normal (LO2 293T) comparison cisplatin, indicating that can potentially be used therapy. On other hand, upgraded expression levels IFN-β vivo preventing from hydrolyzing cGAMP stimulate more potent response. Therefore, might applied boost antitumor immunity for immunotherapy. Overall, our work provides development promising drug

Language: Английский

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Editorial of Special Issue “Protective and Detrimental Role of Heme Oxygenase-1”: 2021

International Journal of Molecular Sciences, Journal Year: 2023, Volume and Issue: 24(5), P. 4386 - 4386

Published: Feb. 23, 2023

The Special Issue “Protective and detrimental role of heme oxygenase-1”(2021), in the International Journal Molecular Sciences, includes original research papers reviews aiming to understand protective or HO-1 signaling pathway involved [...]

Language: Английский

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Spirooxindole derivatives as an anticancer agent

Elsevier eBooks, Journal Year: 2024, Volume and Issue: unknown, P. 411 - 438

Published: Jan. 1, 2024

Language: Английский

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