ChemInform Abstract: New Pyrazolinylanilinoquinolines and Other Related Products of Possible Antibacterial Activity.

Kamel, Mona M.; Nabih, I.; Gadalla, K. Z.; Ashour, M. M.

doi:10.1002/chin.198624208

Cited by 4 publications

(5 citation statements)

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“…HCl as described by Ashour et al for (IIIa) [19]. Compound (IIIb) showed a broad band for the N at 3375 cm -1 , IR spectrum, as well as a bathochromic shifted band at 1660 cm -1 for the aro matic C=O group.…”

Section: Resultsmentioning

confidence: 96%

Synthesis of some quinolinyl chalcone analogues and investigation of their anticancer and synergistic anticancer effect with doxorubicin

et al. 2012

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Two derivatives of 2-(4-acetylanilino)quinolines (IIIa, b) were synthesized as scaffolds for synthesis of open chalcone analogues (Va-f) through Claisen-Schmidt condensation with a set of aromatic aldehydes (IVa-d). Derivatives (Va, b) were further manipulated into cyclic alpha,beta-unsaturated ketones by Michael-addition of acetylacetone and ethylacetoacetate affording derivatives (VI-VII). Deethoxycarboxylation of derivatives (VIIa, b) afforded cyclohexenons (VIIIa, b) allowing formation of a mini library of alpha,beta-unsaturated ketones for screening their anticancer and synergistic anticancer effect with doxorubicin using colon cancer cell line (Caco-2). Two open enones, (Vb) and (Ve), showed significant anticancer activity with IC50 of 5.0 and 2.5 microM respectively. Only one cyclic enone, (VIa) showed synergistic anticancer activity with doxorubicin at 10 microM.

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Section: Resultsmentioning

confidence: 96%

Synthesis of some quinolinyl chalcone analogues and investigation of their anticancer and synergistic anticancer effect with doxorubicin

et al. 2012

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“…In addition, chalcones serve as intermediates for the synthesis of corresponding pyrazolines by undergo a subsequent cyclization reaction with hydrazine hydrate, which are found to have extensive pharmaceutical applications. [51][52][53] So, N-(3-(2-hydroxyphenyl)acryloyl)phthalimide 1 was treated with hydrazine hydrate in ethanol to afford N-(5-(2-hydroxyphenyl)-4,5-dihydro-1H-pyrazol-3-yl)phthalimide (HPZPHT) 2 in 80 % yield.…”

Section: Resultsmentioning

confidence: 99%

Synthesis, radioiodination and biological evaluation of a novel phthalimide derivative

Motaleb

Abdel-Ghaney

Abdel‐Bary

et al. 2015

J Radioanal Nucl Chem

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Biologically active novel phthalimide derivative, N-(5-(2-hydroxyphenyl)-4,5-dihydro-1H-pyrazol-3-yl)phthalimide (HPZPHT), was synthesized in excellent yield and characterized by IR, mass and 1 H NMR spectroscopy. It was radiolabeled with iodine-131 by direct electrophilic substitution reaction and radiochemical yield was determined by using different chromatographic techniques (HPLRC, paper chromatography and paper electrophoresis). 131 I-HPZPHT has high radiolabeling yield (98.00 ± 2.00 %), stability, solid tumor uptake and T/NT ratio (5.17 ± 0.03 at 30 min. post-injection) compared with many new tracers which have been developed in recent years. This study encourages the possible use of this tracer as a potential imaging and/or therapeutic agent for cancer.

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“…e compounds with heterocyclic core structures are pharmaceutically important class of compounds because of their diverse range of biological importance such as anticancer activity against cancer cell lines [6,7]. In view of the facts mentioned above and as a part of our efforts to identify new anticancer drug candidates [16], a ChemBank ™ library of 2344 small molecules with an anticancer activity was downloaded [17] for specific docking.…”

Section: Molecular Docking Analysis and Admet Profilementioning

confidence: 99%

“…Heterocyclic compounds have been found to gain extensive interest due to their considerable wide range applications in medicinal, pharmaceutical, and pharmacological activities especially as anticancer agents [6,7]. In the present study, computer aided virtual screening studies were carried out using ChemBank ™ database to report new molecular entities which can be used as potent inhibitors against MLAA-42 protein.…”

Section: Introductionmentioning

confidence: 99%

Homology Modeling and Virtual Screening Studies of Antigen MLAA-42 Protein: Identification of Novel Drug Candidates against Leukemia—An In Silico Approach

Shehadi

Rashdan

Abdelmonsef

2020

Computational and Mathematical Methods in Medicine

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Monocytic leukemia-associated antigen-42 (MLAA-42) is associated with excessive cell division and progression of leukemia.us, human MLAA-42 is considered as a promising target for designing of new lead molecules for leukemia treatment. Herein, the 3D model of the target was generated by homology modeling technique. e model was then evaluated using various cheminformatics servers. Moreover, the virtual screening studies were performed to explore the possible binding patterns of ligand molecules to MLAA's active site pocket. irteen ligand molecules from the ChemBank ™ database were identified as they showed good binding affinities, scaffold diversity, and preferential ADME properties which may act as potent drug candidates against leukemia. e study provides the way to identify novel therapeutics with optimal efficacy, targeting MLAA-42.

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ChemInform Abstract: New Pyrazolinylanilinoquinolines and Other Related Products of Possible Antibacterial Activity.

Cited by 4 publications

References 0 publications

Synthesis of some quinolinyl chalcone analogues and investigation of their anticancer and synergistic anticancer effect with doxorubicin

Synthesis of some quinolinyl chalcone analogues and investigation of their anticancer and synergistic anticancer effect with doxorubicin

Synthesis, radioiodination and biological evaluation of a novel phthalimide derivative

Homology Modeling and Virtual Screening Studies of Antigen MLAA-42 Protein: Identification of Novel Drug Candidates against Leukemia—An In Silico Approach

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