Perihan A Elzahhar, Rana A Alaaeddine, Rasha Nassra, Azza Ismail, Hala F Labib, Mohamed G Temraz, Ahmed S F Belal, Ahmed F El-Yazbi,
The work reported herein describes the synthesis of a new series of anti-inflammatory pyrazolyl thiazolones. In addition to COX-2/15-LOX inhibition, these hybrids exerted their anti-inflammatory actions through novel mechanisms. The most active compounds possessed COX-2 inhibitory activities comparable to celecoxib (IC<sub>50</sub> values of 0.09-0.14 µM) with significant 15-LOX inhibitory activities (IC<sub>50</sub>s ... Read more >>
J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2021, 36(1):669-684]
Cited: 0 times
Ibrahim Chaaban, Haidy Hafez, Ibrahim AlZaim, Cynthia Tannous, Hanan Ragab, Aly Hazzaa, Salma Ketat, Asser Ghoneim, Mohamed Katary, Mohammad M Abd-Alhaseeb, Fouad A Zouein, Amgad Albohy, Ahmed Noby Amer, Ahmed F El-Yazbi, Ahmed S F Belal,
We managed to repurpose the old drug iodoquinol to a series of novel anticancer 7-iodo-quinoline-5,8-diones. Twelve compounds were identified as inhibitors of moderate to high potency on an inhouse MCF-7 cell line, of which 2 compounds (5 and 6) were capable of reducing NAD level in MCF-7 cells in concentrations ... Read more >>
Bioorg Chem (Bioorganic chemistry)
[2021, 113:105035]
Cited: 0 times
Rana A Alaaeddine, Perihan A Elzahhar, Ibrahim AlZaim, Wassim Abou-Kheir, Ahmed S F Belal, Ahmed F El-Yazbi,
Emerging evidence supports an intertwining framework for the involvement of different inflammatory pathways in a common pathological background for a number of disorders. Of importance are pathways involving arachidonic acid metabolism by cyclooxygenase-2 (COX-2) and 15-lipoxygenase (15-LOX). Both enzyme activities and their products are implicated in a range of pathophysiological ... Read more >>
Curr Med Chem (Current medicinal chemistry)
[2021, 28(11):2260-2300]
Cited: 2 times
Perihan A Elzahhar, Shrouk M Abd El Wahab, Mohamed Elagawany, Hoda Daabees, Ahmed S F Belal, Ahmed F El-Yazbi, Ali H Eid, Rana Alaaeddine, Rehab R Hegazy, Rasha M Allam, Maged W Helmy, Bahaa Elgendy, Andrea Angeli, Soad A El-Hawash, Claudiu T Supuran,
Cancer is a multifactorial disorder involving multiplicity of interrelated signaling pathways and molecular targets. To that end, a multi-target design strategy was adopted to develop some 1,2,3-triazoles hybridized with some pharmacophoric anticancer fragments, as first-in-class simultaneous inhibitors of COX-2, 15-LOX and tumor associated carbonic anhydrase enzymes. Results revealed that compounds ... Read more >>
Eur J Med Chem (European journal of medicinal chemistry)
[2020, 200:112439]
Cited: 3 times
Ehab D AlFadly, Perihan A Elzahhar, Anna Tramarin, Salwa Elkazaz, Hossam Shaltout, Marwa M Abu-Serie, Jana Janockova, Ondrej Soukup, Doaa A Ghareeb, Ahmed F El-Yazbi, Rim W Rafeh, Nour-Mounira Z Bakkar, Firas Kobeissy, Isabel Iriepa, Ignacio Moraleda, Manal N S Saudi, Manuela Bartolini, Ahmed S F Belal,
Neuroinflammation and cholinergic deficit are key detrimental processes involved in Alzheimer's disease. Hence, in the search for novel and effective treatment strategies, the multi-target-directed ligand paradigm was applied to the rational design of two series of new hybrids endowed with anti-inflammatory and anticholinesterase activity via triple targeting properties, namely able ... Read more >>
Eur J Med Chem (European journal of medicinal chemistry)
[2019, 167:161-186]
Cited: 7 times
Perihan A Elzahhar, Rana Alaaeddine, Tamer M Ibrahim, Rasha Nassra, Azza Ismail, Benjamin S K Chua, Rebecca L Frkic, John B Bruning, Nadja Wallner, Tilo Knape, Andreas von Knethen, Hala Labib, Ahmed F El-Yazbi, Ahmed S F Belal,
In search for effective multi-targeting drug ligands (MTDLs) to address low-grade inflammatory changes of metabolic disorders, we rationally designed some novel glitazones-like compounds. This was achieved by incorporating prominent pharmacophoric motifs from previously reported COX-2, 15-LOX and PPARγ ligands. Challenging our design with pre-synthetic docking experiments on PPARγ showed encouraging ... Read more >>
Eur J Med Chem (European journal of medicinal chemistry)
[2019, 167:562-582]
Cited: 6 times
Perihan Elzahhar, Ahmed S F Belal, Fatema Elamrawy, Nada A Helal, Mohamed Ismail Nounou,
For the past three decades, pharmaceutical research has been mainly converging to novel carrier systems and nanoparticulate colloidal technologies for drug delivery, such as nanoparticles, nanospheres, vesicular systems, liposomes, or nanocapsules to impart novel functions and targeting abilities. Such technologies opened the gate towards more sophisticated and effective multi-acting platform(s) ... Read more >>
Methods Mol Biol (Methods in molecular biology (Clifton, N.J.))
[2019, 2000:125-182]
Cited: 3 times
Mohamed G Temraz, Perihan A Elzahhar, Alaa El-Din A Bekhit, Adnan A Bekhit, Hala F Labib, Ahmed S F Belal,
Leishmaniasis is a devastating tropical disease with limited therapeutic options. Depending on recently reported active anti-leishmanial compounds, we designed and synthesized a series of click modifiable 1,2,3-triazole and thiosemicarbazone hybrids. Most of the synthesized compounds showed comparable to superior activity to a well-established anti-leishmanial drug miltefosine. Compounds 2 and 10a ... Read more >>
Eur J Med Chem (European journal of medicinal chemistry)
[2018, 151:585-600]
Cited: 6 times
Ghandoura Moussa, Rana Alaaeddine, Lynn M Alaeddine, Rasha Nassra, Ahmed S F Belal, Azza Ismail, Ahmed F El-Yazbi, Yasser S Abdel-Ghany, Aly Hazzaa,
Click chemistry was used to synthesize a new series of thioquinazolinone molecules equipped with propargyl moiety,1,2,3-triazolyl and isoxazolyl rings. Our design was based on merging pharmacophores previously reported to exhibit COX-2 inhibitory activities to a thioquinazolinone-privileged scaffold. The synthesized compounds were subjected to in vitro cyclooxygenase COX-1/COX-2 and 15-LOX inhibition assays. ... Read more >>
Eur J Med Chem (European journal of medicinal chemistry)
[2018, 144:635-650]
Cited: 6 times