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Design and synthesis of uracil/thiouracil based quinoline scaffolds as topoisomerases I&II inhibitors for chemotherapy: A new hybrid navigator with DFT calculation
Faculty
Pharmacy
Year:
2023
Type of Publication:
ZU Hosted
Pages:
Authors:
Samar Saied Mahmoud Mohamed Elbaramawy
Staff Zu Site
Abstract In Staff Site
Journal:
bioorganic Chemistry ElSevier
Volume:
Keywords :
Design , synthesis , uracil/thiouracil based quinoline scaffolds
Abstract:
In this work, a novel promising hybrid mode of uracil/thiouracil based quinoline pharmacophore i.e. 5a-f was rationalized and synthesized based on rigidification and lipophilic principles, and following the reported pharmacophoric features of camptothecin & doxorubicin. Concurrently, a non-rigid mode pharmacophore i.e. 7a-f was also designed and synthesized. The anti-proliferative activity of the compounds was assessed against three different cancer cell lines, namely A549 lung cancer, MCF-7 breast adenocarcinoma, and HepG-2 hepatic carcinoma. Further, promising candidates were evaluated against A549, and MCF-7 and for their ability to inhibit topoisomerases I &II. Compound 5f was observed to be the most active congener, displaying the highest cell inhibition of 84.4% for topoisomerase I and 92%, for topoisomerase II at a concentration of 100 µM. When its cytotoxicity was evaluated against A549 cells, 5f arrested the cell cycle at the S phase and increased the apoptosis ratio by 46.31%. DFT calculation of 5f showed higher dipole moment and greater negative energy values (-247531.510 kcal/mol) with positive & negative poles, and better stability reflection. Furthermore, molecular docking of 5f to both enzymes showed good agreement with the biological assessment. This study has given insight for further consideration of the highly promising hybrid 5f.
Author Related Publications
Samar Saied Mahmoud Mohamed Elbaramawy, "Spectrophotometric determination of ranitidine hydrochloride and famotidine using 1,2- naphthoquinone-4-sulphonate", Zagazig, 2013
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Samar Saied Mahmoud Mohamed Elbaramawy, "RP-HPLC method for the simultaneous determination of omeprazole, tinidazole and doxycycline mixture in the presence of omeprazole and tinidazole degradation products", Academic Sciences, India, 2014
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Samar Saied Mahmoud Mohamed Elbaramawy, "Validated spectophotometric determination of pantoprazole sodium in tablets using 2,4-dinitrofluorobenzene through nucleophilic substitution reaction", India, 2014
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Samar Saied Mahmoud Mohamed Elbaramawy, "Spectrophotometric determination of omeprazole via nitrosation reaction", Academic Sciences, India, 2014
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Samar Saied Mahmoud Mohamed Elbaramawy, "Spectrophotometric determination of omeprazole sodium and rantidine hydrochloride using 2,4-dinitrofluorobenzene and 4-chloro-7-nitrobenz-2-oxa-1,3-diazole accompanied with a kinetic study", America, 2014
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Department Related Publications
Mohamed Gamal Helmy Mohamed Abdelwahed, "Electronic Properties of Organic Complexes. 2. Reactive Azodyes", Spain, 1993
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Hamdy Aldedamony , "Studies on Portland Blast-Furnace Slag Cement with Limestone as a Retarder”", Indian J. Eng. & Sci, 1995
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Hamdy Aldedamony , "Resistivity of an Artificial Pozzolanic Cement to Chloride Solutions”", Silic. Ind.,, 1994
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Ragaa Sheikh Shuhaib, "Utility of Oxidation-Reduction Reaction for Determination of Gemifloxacin Mesylate and Moxifloxacin HCl in Pure Form and in Pharmaceutical Formulations using N-Bromosuccinimide", OMICS Publishing Group, 2013
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Ayman AboulFotouh Gouda Sallem, "Spectophotometricmethods for determination of cefdinir in pharmaceutical formulations via derivatization with 1,2-naphthoquinone-4-sulfonate and 4-chloro-7-nitrobenzo-2-oxa-1, 3-diazole", Wiley Online Library, 2011
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