Full Text Journal Articles by
Author Aly Hazzaa

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Transforming iodoquinol into broad spectrum anti-tumor leads: Repurposing to modulate redox homeostasis.

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

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Discovery of small molecule acting as multitarget inhibitor of colorectal cancer by simultaneous blocking of the key COX-2, 5-LOX and PIM-1 kinase enzymes.

Mostafa M M El-Miligy, Ahmed K Al-Kubeisi, Saad R El-Zemity, Rasha A Nassra, Marwa M Abu-Serie, Aly A Hazzaa,

Colorectal cancer (CRC) is the second cause of cancer death worldwide. Inhibitors of COX-2, 5-LOX and PIM-1 kinase were very effective in the treatment and prevention of CRC in mouse models in vivo. Furthermore, thymol was confirmed to inhibit CRC cell proliferation in cancer cell lines and inhibitory activity against ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 115:105171]

Cited: 1 time

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New pyrimidines and triazolopyrimidines as antiproliferative and antioxidants with cyclooxygenase-1/2 inhibitory potential.

Ashraf M Omar, Heba A Abd El Razik, Aly A Hazzaa, Maryam Az El-Attar, Maha A El Demellawy, Abeer E Abdel Wahab, Soad Am El Hawash,

<b>Aim:</b> Cyclooxygenase-2 (COX-2) inhibition and scavenging-free radicals are important targets in cancer treatment. <b>Materials & methods:</b> Sulfanylpyrimidines and triazolopyrimidines were synthesized and evaluated as anticancer and antioxidant COX-1/2 inhibitors. <b>Results:</b> Compound <b>7</b> showed the same growth inhibitory activity as 5-fluorouracil against MCF-7. Compound <b>6f</b> displayed broad-spectrum anticancer activity against the ... Read more >>

Future Med Chem (Future medicinal chemistry)
[2019, 11(13):1583-1603]

Cited: 1 time

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Synthesis, antibacterial evaluation, and DNA gyrase inhibition profile of some new quinoline hybrids.

Ola H Rizk, Mohamed G Bekhit, Aly A B Hazzaa, El-Sayeda M El-Khawass, Ibrahim A Abdelwahab,

Antibiotic-resistant bacteria continue to play an important role in human health and disease. Inventive strategies are necessary to develop new therapeutic leads to challenge drug-resistance problems. From this perception, new quinoline hybrids bearing bioactive pharmacophores were synthesized. The newly synthesized compounds were evaluated for their in vitro antibacterial activity against ... Read more >>

Arch Pharm (Weinheim) (Archiv der Pharmazie)
[2019, 352(10):e1900086]

Cited: 0 times

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Design, synthesis and docking study of pyridine and thieno[2,3-b] pyridine derivatives as anticancer PIM-1 kinase inhibitors.

Marwa E Abdelaziz, Mostafa M M El-Miligy, Salwa M Fahmy, Mona A Mahran, Aly A Hazzaa,

A series of pyridine and thieno[2,3-b]pyridine derivatives have been designed and synthesized as anticancer PIM-1 kinase inhibitors. Thirty-seven compounds were selected by NCI to be tested initially at a single dose (10 µM) in the full NCI 60 cell line panel. Compound 5b showed potent anticancer activity and was tested twice ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2018, 80:674-692]

Cited: 2 times

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Novel click modifiable thioquinazolinones as anti-inflammatory agents: Design, synthesis, biological evaluation and docking study.

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

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New benzothiophene derivatives as dual COX-1/2 and 5-LOX inhibitors: synthesis, biological evaluation and docking study.

Mostafa Mm El-Miligy, Aly A Hazzaa, Hanan El-Messmary, Rasha A Nassra, Soad Am El-Hawash,

<h4>Aim</h4>Simultaneous inhibition of 5-LOX/COX may enhance anti-inflammatory effects and reduce side effects. Hence, synthesis of novel dual inhibitors of 5-LOX/COX is an important strategy for treatment of inflammation. Results/methodology: The target compounds were designed to hybridize benzothiophene scaffold or its bioisostere benzofuran with various anti-inflammatory pharmacophore hetercycles through different atoms ... Read more >>

Future Med Chem (Future medicinal chemistry)
[2017, 9(5):443-468]

Cited: 2 times

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New hybrid molecules combining benzothiophene or benzofuran with rhodanine as dual COX-1/2 and 5-LOX inhibitors: Synthesis, biological evaluation and docking study.

Mostafa M M El-Miligy, Aly A Hazzaa, Hanan El-Messmary, Rasha A Nassra, Soad A M El-Hawash,

New molecular hybrids combining benzothiophene or its bioisostere benzofuran with rhodanine were synthesized as potential dual COX-2/5-LOX inhibitors. The benzothiophene or benzofuran scaffold was linked at position -2 with rhodanine which was further linked to various anti-inflammatory pharmacophores so as to investigate the effect of such molecular variation on the ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2017, 72:102-115]

Cited: 7 times

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Synthesis of novel benzofuran and related benzimidazole derivatives for evaluation of in vitro anti-HIV-1, anticancer and antimicrobial activities.

Samia M Rida, Soad A M El-Hawash, Hesham T Y Fahmy, Aly A Hazzaa, Mostafa M M El-Meligy,

Previously, we synthesized and evaluated several benzofuran derivatives containing heterocyclic ring substituents linked to the benzofuran nucleus at C-2 by a two- to four-atom spacer as potential anti-HIV-1, anticancer and antimicrobial agents. Among these derivatives, NSC 725612 and NSC 725716 exhibited interesting anti-HIV-1 activity. To further investigate the structure-activity relationship, ... Read more >>

Arch Pharm Res (Archives of pharmacal research)
[2006, 29(10):826-833]

Cited: 27 times

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