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Quinazoline‐tethered hydrazone: A versatile scaffold toward dual anti‐TB and EGFR inhibition activities in NSCLC
Faculty
Pharmacy
Year:
2021
Type of Publication:
ZU Hosted
Pages:
Authors:
Hend Kather Abdelhakem Elhamalawy
Staff Zu Site
Abstract In Staff Site
Journal:
Archiv der pharmazie wiley
Volume:
Keywords :
Quinazoline‐tethered hydrazone: , versatile scaffold toward dual anti‐TB
Abstract:
Globally, lung cancer and tuberculosis are considered to be very serious and complex diseases. Evidence suggests that chronic infection with tuberculosis (TB) can often lead to lung tumors; therefore, developing drugs that target both diseases is of great clinical significance. In our study, we designed and synthesized a suite of 14 new quinazolinones (5a–n) and performed biological investigations of these compounds in Mycobacterium tuberculosis (MTB) and cancer cell lines. In addition, we conducted a molecular modeling study to determine the mechanism of action of these compounds at the molecular level. Compounds that showed anticancer activity in the preliminary screening were further evaluated in three cancer cell lines (A549, Calu‐3, and BT‐474 cells) and characterized in an epidermal growth factor receptor (EGFR) binding assay. Cytotoxicity in noncancerous lung fibroblast cells was also evaluated to obtain safety data. Our theoretical and experimental studies indicated that our compounds showed a mechanism of action similar to that of erlotinib by inhibiting the EGFR tyrosine kinase. In turn, the antituberculosis activity of these compounds would be produced by the inhibition of enoyl‐ACP‐reductase. From our findings, we were able to identify two potential lead compounds (5i and 5l) with dual activity and elevated safety toward noncancerous lung fibroblast cells. In addition, our data identified three compounds with excellent anti‐TB activities (compounds 5i, 5l, and 5n).
Author Related Publications
Hend Kather Abdelhakem Elhamalawy, "Preclinical evaluation of Rad6 inhibition to overcome platinum resistance in ovarian cancer", AACR, 2016
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Hend Kather Abdelhakem Elhamalawy, "Design, synthesis and in vitro anticancer evaluation of 4,6-diamino-1,3,5-triazine-2-carbohydrazides and -carboxamides", ELSEVIER, 2013
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Hend Kather Abdelhakem Elhamalawy, "Synthesis of New 2,3-Dihydroquinazolin-4(1H)-one Derivatives for Analgesic and Anti-inflammatory Evaluation", WILEY interscience, 2010
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Hend Kather Abdelhakem Elhamalawy, "Synthesis of new benzotriazepin-5(2H)-one derivatives of expected antipsychotic activity", springer link, 2013
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Hend Kather Abdelhakem Elhamalawy, "Novel Inhibitors of Rad6 Ubiquitin Conjugating Enzyme: Design, Synthesis, Identification, and Functional Characterization", AACR publications, 2013
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Department Related Publications
Abdallah Ahmed Abdallah Elshanawany, "Development and validation of liquid chromatographic method for simultaneous determination of amiloride hydrochloride and hydrochlorothiazide in human urine", لايوجد, 1900
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Abdallah Ahmed Abdallah Elshanawany, "HPLC Determination of polymyxin sulphate, Benzalkonium chloride, and gramicidine in pharm.formulation ", لايوجد, 1900
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Abdallah Ahmed Abdallah Elshanawany, "Synchronous Spectroflurimetric Determination of Famtidine,Fluconazole and Ketoconazole in bulk powder and in pharmaceutical dosages forms ", لايوجد, 1900
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Abdallah Ahmed Abdallah Elshanawany, "Synthesis of 3- substituted (6-bromo-2-imidazo{4,5-b}pyridinyl)propionic acid as antiinflammatory agents. ", لايوجد, 1900
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Abdallah Ahmed Abdallah Elshanawany, "Application of difference spectrophotometry to the nitrosation reaction in the assay of certain antipyretic drugs . ", لايوجد, 1900
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