Hatem A. Abdel-Aziz
Cairo University
Hydrogen bondCrystal structureMedicinal chemistryOrganic chemistryChemistryApoptosisIn vitroCombinatorial chemistryCarbonic anhydraseBenzofuranIsatinPyrazoleBenzeneBenzimidazoleRing (chemistry)CrystalBioinformaticsStereochemistryCrystallographyDihedral angle
225Publications
32H-index
3,034Citations
Publications 209
Newest
#1Wagdy M. Eldehna (Kafrelsheikh University)H-Index: 25
#2Rofaida Salem (Kafrelsheikh University)H-Index: 1
Last. Hatem A. Abdel-AzizH-Index: 32
view all 11 authors...
In the current work, a new set of carbohydrazide linked benzofuran-isatin conjugates (5a-e and 7a-i) was designed and synthesised. The anticancer activity for compounds (5b-d, 7a, 7b, 7d and 7g) was measured against NCI-55 human cancer cell lines. Compound 5d was the most efficient, and thus subjected to the five-dose screen where it showed excellent broad activity against almost all tested cancer subpanels. Furthermore, all conjugates (5a-e and 7a-i) showed a good anti-proliferative activity to...
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#1Wagdy M. Eldehna (Kafrelsheikh University)H-Index: 25
#2Mahmoud F. Abo-Ashour (Egyptian Russian University)H-Index: 9
Last. Radwan El-Haggar (Helwan University)H-Index: 6
view all 11 authors...
Mitochondrial anti-apoptotic Bcl2 and BclxL proteins, are overexpressed in multiple tumour types, and has been involved in the progression and survival of malignant cells. Therefore, inhibition of ...
2 CitationsSource
#1Diaaeldin M. Elimam (University of Bradford)
#2Abdullah A. Elgazar (Kafrelsheikh University)H-Index: 4
Last. Wagdy M. Eldehna (Kafrelsheikh University)H-Index: 25
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Abstract null null The natural product piperine, the major bioactive alkaloid present in black pepper fruits, has the ability to modulate the functional activity of several biological targets. In this study, we have utilized the natural piperine as a tail moiety to develop new SLC-0111 analogues (6a-d, 8 and 9) as potential carbonic anhydrase inhibitors. Thereafter, different functionalities, free carboxylic acid (11a-c), acetyl (13a) and ethyl ester (13b-c), were exploited as bioisosteres of th...
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#1Assem H. Eldeeb (Egyptian Russian University)
#2Mahmoud F. Abo-Ashour (Egyptian Russian University)H-Index: 9
Last. Claudiu T. Supuran (UniFI: University of Florence)H-Index: 152
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Abstract New series of benzenesulfonamide and benzoic acid derivatives were designed and synthesized using tail/dual tail approach to improve potency and selectivity as carbonic anhydrase inhibitors. The synthesized compounds evaluated as CAIs against isoforms hCA I, II, IV and IX with AAZ as standard inhibitor. The benzenesulfonamide derivatives 7a-d, 8a-h, 12a-c, 13a and 15a-c showed moderate to potent inhibitory activity with selectivity toward isoform hCA II, especially, compound 13a with (K...
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#1Moataz A. Shaldam (Kafrelsheikh University)H-Index: 4
#2Wagdy M. Eldehna (Kafrelsheikh University)H-Index: 25
Last. Claudiu T. Supuran (UniFI: University of Florence)H-Index: 152
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Abstract In the present study, we describe the design of different series of benzofuran-based derivatives as potential carbonic anhydrase inhibitors (CAIs). The adopted design is based on bioisosteric replacement for the p-fluorophenyl SLC-0111 tail with the lipophilic 2-methylbenzofuran or 5-bromobenzofuran tails to furnish the 2-methylbenzofuran (MBF) sulfonamides (MBFS; 9, 11 and 13) and 5-bromobenzofuran (BBF) sulfonamides (BBFS; 27a-b, 28a-b and 29a-c), respectively. Thereafter, the urea sp...
7 CitationsSource
#1Mostafa M. Elbadawi (Hiroshima University)H-Index: 1
#2Wagdy M. Eldehna (Kafrelsheikh University)H-Index: 25
Last. Mohammad M. Al-SaneaH-Index: 11
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ABSTRACT As a front-runner selective CA IX inhibitor currently in Phase Ib/II clinical trials, SLC-0111 has been herein exploited as a lead molecule for development of new different sets of N-phenyl-2-(phenylsulfonyl)acetamides/propanamides incorporating different functionalities; primary sulfonamide (5a-f), free carboxylic (8a, 8d), ethyl ester (8b, 8e), acetyl (8c, 8f) and nitro (10a, 10b), as potential carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. All the prepared analogues have been examin...
3 CitationsSource
#1Wagdy M. Eldehna (Kafrelsheikh University)H-Index: 25
Last. Radwan El-Haggar (Helwan University)H-Index: 6
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Abstract In the current medical era, human health is experiencing numerous challenges, particularly the human malignancies. Therefore, the therapeutic arsenal for these malignancies is to be inexorably enhanced with new treatments that target tumor cells in a selective manner. In this regard, the present work aims at developing a new set of small molecules featuring the privileged isatin scaffold conjugated with a thiazolo[3,2-a]benzimidazole (TBI) motif through a cleavable hydrazide linker (7a-...
2 CitationsSource
#1Zainab M. Elsayed (Kafrelsheikh University)H-Index: 4
#2Wagdy M. Eldehna (Kafrelsheikh University)H-Index: 25
Last. Eman R. Mohammed (Cairo University)H-Index: 3
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Joining the global fight against Tuberculosis, the world's most deadly infectious disease, herein we present the design and synthesis of novel isatin-nicotinohydrazide hybrids (5a–m and 9a–c) as pr...
2 CitationsSource
In this study, diverse series of coumarin derivatives were developed as potential carbonic anhydrase inhibitors (CAIs). A "tail" approach was adopted by selecting the coumarin motif as a tail that is connected to the ZBG benzenesulfonamide moiety via a hydrazine (4a,b) or hydrazide (5a,b) linker. Thereafter, an aryl sulfone tail was incorporated to afford the dual tailed coumarin-sulfonamide arylsulfonehydrazones (13a-d) and hydrazides (14a,b). Then, the ZBG were removed from compounds 13 and 14...
5 CitationsSource
#1Tarek A. Yousef (Islamic University)H-Index: 23
#2Essam EzzeldinH-Index: 11
Last. Gamal A. E. MostafaH-Index: 15
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Background Electron donor-acceptor interactions are important molecular reactions for the activity of pharmacological compounds. The aim of the study is to develop a charge transfer (CT) complex: synthesis, characterization, antimicrobial activity, and theoretical study. Method and results A solid CT complex of neostigmine (NSG) with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ) was synthesized and characterized by infrared spectra, NMR, and UV-visible spectroscopy. The results confirm the for...
2 CitationsSource