Activated Anilide in Heterocyclic Synthesis: Synthesis of New Dihydropyridines, Dihydropyridazines and Thiourea Derivatives

Hafiz, Ibrahim Saad Abdel; Ramiz, M. M. M.; Sarhan, Ahmed A. M.

doi:10.1002/cjoc.201190216

Cited by 3 publications

(1 citation statement)

References 31 publications

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“…For example, the 1 H NMR spectrum of 5a showed the presence of a multiple signal at δ = 7.14 − 8.90 ppm corresponding to aromatic protons and two signals at δ = 11.77 and 14.72 ppm corresponding to two NH groups, It should be emphasized here that the signal corresponding to amino function of hydrazo group appears at downfield at δ = 14.72 ppm due to the intramolecular hydrogen bonding with carbonyl group. 30 The IR spectrum of the same product further supports the hydrozo structure. Fusion of aryl hydrazones 5a-d with malononitrile in domestic microwave oven for 3 min afforded the dihydropyridazines 7a-d via intermediacy of 6a-d (scheme 1).…”

Section: Resultsmentioning

confidence: 60%

Activated anilide in heterocyclic synthesis: Synthesis of new hydrazo, dihydropyridazine, tetrahydropyridine, dihydropyridine and pyranopyridine derivatives

Hafiz

Ramiz²,

Elian

2012

J Chem Sci

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A series of new hydrazo, dihydropyridazine, tetrahydropyridine, dihydropyridine and pyranopyridine derivatives with known biological activity have been prepared through the reactions of 3-oxo-3-phenyl-N-(pyridine-3-yl) propanamide 3 and enaminonitrile 17 with some electrophilic reagents, nucleophilic reagents, and aryl diazonium salts. The newly synthesized compounds were characterized by IR, 1 H NMR and mass spectral studies.

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Section: Resultsmentioning

confidence: 60%

Activated anilide in heterocyclic synthesis: Synthesis of new hydrazo, dihydropyridazine, tetrahydropyridine, dihydropyridine and pyranopyridine derivatives

Hafiz

Ramiz²,

Elian

2012

J Chem Sci

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ChemInform Abstract: Activated Anilide in Heterocyclic Synthesis: Synthesis of New Dihydropyridines (IV), Dihydropyridazines (VIII) and Thiourea Derivatives (X).

2011

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<p>Virtual Screening and Optimization of Novel mTOR Inhibitors for Radiosensitization of Hepatocellular Carcinoma</p>

Feng¹,

Gu²,

Yong-Shou³

et al. 2020

DDDT

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Background: Radiotherapy has an ameliorative effect on a wide variety of tumors, but hepatocellular carcinoma (HCC) is insensitive to this treatment. Overactivated mammalian target of rapamycin (mTOR) plays an important part in the resistance of HCC to radiotherapy; thus, mTOR inhibitors have potential as novel radiosensitizers to enhance the efficacy of radiotherapy for HCC. Methods: A lead compound was found based on pharmacophore modeling and molecular docking, and optimized according to the differences between the ATP-binding pockets of mTOR and PI3K. The radiosensitizing effect of the optimized compound (2a) was confirmed by colony formation assays and DNA double-strand break assays in vitro. The discovery and preclinical characteristics of this compound are described. Results: The key amino acid residues in mTOR were identified, and a precise virtual screening model was constructed. Compound 2a, with a 4,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidine scaffold, exhibited promising potency against mTOR (mTOR IC 50 =7.1 nmol/L (nM)) with 126-fold selectivity over PI3Kα. Moreover, 2a significantly enhanced the sensitivity of HCC to radiotherapy in vitro in a dose-dependent manner. Conclusion: A new class of selective mTOR inhibitors was developed and their radiosensitization effects were confirmed. This study also provides a basis for developing mTORspecific inhibitors for use as radiosensitizers for HCC radiotherapy.

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Activated Anilide in Heterocyclic Synthesis: Synthesis of New Dihydropyridines, Dihydropyridazines and Thiourea Derivatives

Cited by 3 publications

References 31 publications

Activated anilide in heterocyclic synthesis: Synthesis of new hydrazo, dihydropyridazine, tetrahydropyridine, dihydropyridine and pyranopyridine derivatives

Activated anilide in heterocyclic synthesis: Synthesis of new hydrazo, dihydropyridazine, tetrahydropyridine, dihydropyridine and pyranopyridine derivatives

ChemInform Abstract: Activated Anilide in Heterocyclic Synthesis: Synthesis of New Dihydropyridines (IV), Dihydropyridazines (VIII) and Thiourea Derivatives (X).

<p>Virtual Screening and Optimization of Novel mTOR Inhibitors for Radiosensitization of Hepatocellular Carcinoma</p>

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