mamdouh.fawzi

Mamdouh Fawzy Ahmed Mohamed

Lecturer - Lecturer of Pharmaceutical Chemistry, Head of Pharmaceutical Chemistry Department Lab and Co-ordinate of Clinical Pharmacy Program

Faculty of Pharmacy

Address: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sohag University, 82524 Sohag, Egypt

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Design, synthesis and anticancer activity of novel valproic acid conjugates with improved histone deacetylase (HDAC) inhibitory activity

2020 | Keywords Valproic acid; Anticancer;,
Design, synthesis and anticancer activity of novel valproic acid conjugates with improved histone deacetylase (HDAC) inhibitory activity
Twenty-five valproic acid conjugates have been designed and synthesized. All target compounds were explored for their in vitro anti-proliferative activities using the MTT-based assay against four human cancer cell lines includingliver (HePG2), colon (HCT116), breast (MCF7) and cervical (HeLa) carcinoma cell lines. Out of six valproic acid-amino acid conjugates 2a-f. Only cysteine containing conjugate 2f showed the significant activity (IC50 ... Read more

Design, Synthesis and Biological Evaluation of New HDAC1 and HDAC2 Inhibitors Endowed with Ligustrazine as a Novel Cap Moiety

2020 | Keywords HDACs Inhibitors;, Ligustrazine, , Anticancer agents, , In silico study, , Synthesis,
Design, Synthesis and Biological Evaluation of New HDAC1 and HDAC2 Inhibitors Endowed with Ligustrazine as a Novel Cap Moiety
INTRODUCTION: Histone deacetylases (HDACs) represent one of the most validated cancer targets. The inhibition of HDACs has been proven to be a successful strategy for the development of novel anticancer candidates. METHODS: This work describes design and synthesis of a new set of HDAC inhibitors ( 7A-C and 8A, B) utilizing ligustrazine as a novel cap moiety, and achieving the ... Read more

Optimization of the synthesis of het/aryl-amidoximes using an efficient green chemistry

2020 | Keywords Amidoxime;, arylamide;, arylnitrile;, cyanamide;, optimization;, pyrimidine;, 1, 2, 4-oxadiazole,
Optimization of the synthesis of het/aryl-amidoximes using an efficient green chemistry
This work focuses on optimizing an efficient green synthesis of arylamidoximes from appropriate nitrile and hydroxylamine hydrochloride in water and triethylamine (1.6 mol equivalent) as a base at room temperature for 6 h. This new green synthetic methodology is compared with previously known methods. The main advantages of this new process reported are good yield, easier work-up and short reaction ... Read more

Novel aryl carboximidamide and 3-aryl-1,2,4-oxadiazole analogues of naproxen as dual selective COX-2/15-LOX inhibitors: Design, synthesis and docking studies

2019 | Keywords Aryl carboximidamides1, 2, 4-o, Aryl carboximidamides, 1, 2, 4-oxadiazoles, COX-1, COX-2, 15- LOX, Naproxe, anti-inflammatory,
Novel aryl carboximidamide and 3-aryl-1,2,4-oxadiazole analogues of naproxen as dual selective COX-2/15-LOX inhibitors: Design, synthesis and docking studies
A series of novel naproxen analogues containing 3-aryl-1,2,4-oxadiazoles moiety (4B-G) and their reaction intermediates aryl carboximidamides moiety (3B-G) was synthesized and evaluated _in vitro_ as dual COXs/15-LOX inhibitors. Compounds 3B-G exhibited superior inhibitory activity than celecoxib as COX-2 inhibitors. Compounds 3B-D and 3G were the most potent COX-2 inhibitors with IC50 range of 6.4 – 8.13 nM and higher selectivity ... Read more

EGFR inhibitors and apoptotic inducers: Design, synthesis, anticancer activity and docking studies of novel xanthine derivatives carrying chalcone moiety as hybrid molecules

2019 | Keywords Xanthine;, Chalcone;, Hybrids;, EGFRAnti-proliferative;, Apoptotic assay.,
EGFR inhibitors and apoptotic inducers: Design, synthesis, anticancer activity and docking studies of novel xanthine derivatives carrying chalcone moiety as hybrid molecules
One of the helpful ways to improve the effectiveness of anticancer agents and weaken drug resistance is to use hybrid molecules. therefore, the current study intended to introduce 20 novel xanthine/chalcone hybrids 9-28 of promising anticancer activity. Compounds 10, 11, 13, 14, 16, 20 and 23exhibited potent inhibition of cancer cells growth with IC50 ranging from 1.0±0.1 to 3.5±0.4 μM ... Read more

Utilization of tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidinone as a cap moiety in design of novel histone deacetylase inhibitors

2019 | Keywords Tetrahydrobenzo[4, 5]Thieno[2, 3, Histone deacetylase inhibitors, Molecular docking, Anti-proliferative, Apoptotic assay,
Utilization of tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidinone as a cap moiety in design of novel histone deacetylase inhibitors
A series of novel 5,6,7,8-Tetrahydro[1]benzothieno[2,3_-d_]pyrimidin-4(3_H_)-one derivatives bearing a hydroxamic acid, 2-aminoanilide and hydrazide moieties as zinc-binding group (ZBG) were designed, synthesized and evaluated for the HDAC inhibition activity and antiproliferative activity. Most of the tested compounds displayed strong to moderate HDAC inhibitory activity. Some of these compounds showed potent anti-proliferative activity against human HepG2, MCF-7 and HCT-116 cell lines. In ... Read more

Recent Prospectives of Anticancer Histone Deacetylase Inhibitors

2019 | Keywords Multi-targeted HDACIs, Hydroxamic acids, Anticancer;, Shymaa A. Abbass,
Recent Prospectives of Anticancer Histone Deacetylase Inhibitors
Histone deacetylases (HDACs) are common targets for cancer therapy as they are expressed in many forms of cancers; several research studies have been introduced discussing the design of small molecules that target this abnormal epigenetic changes developed by HDACs in chromatin. In the past 10 years, HDAC inhibitors have emerged as important agents of interest in clinical trials for several ... Read more

Antibacterial and Urease Inhibitory activity of New Piperazinyl N-4 Functionalized Ciprofloxacin-oxadiazoles

2019 | Keywords Molecular docking, Urease inhibitors, antibacterial, Oxadiazole, Ciprofloxacin,
Antibacterial and Urease Inhibitory activity of New Piperazinyl N-4 Functionalized Ciprofloxacin-oxadiazoles
This research includes design of new ciprofloxacin bearing oxadiazole at the N-4 piperazinyl for the purpose of having urease inhibitory activity as well as antibacterial activity. Hence, a group of new N-4 piperazinyl oxdiazole derivatives of ciprofloxacin was prepared and characterized using different spectroscopic and analytical techniques including 1H-NMR, 13C-NMR, MS and elemental analysis. Compounds 5b and 5c experienced moderate ... Read more

Design, synthesis, mechanistic and histopathological studies of small- molecules of novel indole-2-carboxamides and pyrazino[1,2-a]indol- 1(2H)-ones as potential anticancer agents effecting the reactive oxygen species production

2018 | Keywords Docking, Anti-cancer,
Design, synthesis, mechanistic and histopathological studies of small- molecules of novel indole-2-carboxamides and pyrazino[1,2-a]indol- 1(2H)-ones as potential anticancer agents effecting the reactive oxygen species production
A series of novel compounds carrying pyrazino[1,2-a]indol-1(2H)-one scaffold (5a-g) and their reac- tion intermediates, indole-2-carboxamides, (3a-g) were synthesized and evaluated for their ability to inhibit reactive oxygen species (ROS) generation, antioxidant activity and anticancer activity against a panel of cancer cell lines using MTT assay. The results showed that these compounds can inhibit ROS generation during the metabolic phase of ... Read more

Novel Pyrrol-2(3 H )-ones and Pyridazin-3(2 H )-ones Carrying Quinoline Scaffold as Anti-proliferative Tubulin Polymerization Inhibitors

2018 | Keywords BRAF Kinase, Tubulin polymerization,
Novel Pyrrol-2(3 H )-ones and Pyridazin-3(2 H )-ones Carrying Quinoline Scaffold as Anti-proliferative Tubulin Polymerization Inhibitors
A novel quinolinyl pyrrolone and quinolinyl pyridazinone derivatives has been synthesized and characterized using different spectroscopic and elemental analysis techniques. Most of the target compounds displayed promising antiproliferative activity; In general, the pyrrolone derivatives 4a-f exhibited higher antiproliferative activity than their corresponding pyridazinone. The pyrrolone 4f showed outstanding antiproliferative activity with moderate selectivity against CNS and renal cancer with selectivity ... Read more