Search Results - "Gomaa, Hesham A.M."

Structure-based design, synthesis and antiproliferative action of new quinazoline-4-one/chalcone hybrids as EGFR inhibitors by Hisham, Mohamed, Hassan, Heba A., Gomaa, Hesham A.M., Youssif, Bahaa G.M., Hayallah, Alaa M., Abdel-Aziz, Mohamed

“…•A series of novel quinazoline-4-one/chalcone hybrids as EGFR inhibitors has been designed and synthesized.•Compounds 19, 20, and 22 were the most active…”
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5-Chlorobenzofuran-2-carboxamides: From allosteric CB1 modulators to potential apoptotic antitumor agents by Youssif, Bahaa G.M., Mohamed, Ashraf M., Osman, Essam Eldin A., Abou-Ghadir, Ola F., Elnaggar, Dina H., Abdelrahman, Mostafa H., Treamblu, Laurent, Gomaa, Hesham A.M.

“…Cannabinoids as THC and the CB1 allosteric modulator CBD were reported to have antiproliferative activities with no reports for other CB1 allosteric modulators…”
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Novel 1,2,4-oxadiazole/pyrrolidine hybrids as DNA gyrase and topoisomerase IV inhibitors with potential antibacterial activity by Frejat, Firas Obaid Arhema, Cao, Yaquan, Zhai, Hongjin, Abdel-Aziz, Salah A., Gomaa, Hesham A.M., Youssif, Bahaa G.M., Wu, Chunli

“…DNA gyrase is a promising target for antibacterial agents. Several classes of small-molecule inhibitors have been discovered in recent decades, but none of…”
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Inhibition of Bruton tyrosine kinase by acalabrutinib dampens lipopolysaccharide/galactosamine-induced hepatic damage by Shaker, Mohamed E., Gomaa, Hesham A.M., Alharbi, Khalid S., Al-Sanea, Mohammad M., El-Mesery, Mohamed E., Hazem, Sara H.

“…[Display omitted] •The effect of the BTK inhibitor acalabrutinib was tested on hepatic damage.•Acalabrutinib inhibited LPS/D-GaIN-induced hepatic injury and…”
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Design, synthesis, crystal structures and biological evaluation of some 1,3-thiazolidin-4-ones as dual CDK2/EGFR potent inhibitors with potential apoptotic antiproliferative effects by Tawfeek, Hendawy N., Hassan, Alaa A., Bräse, S., Nieger, M., Mostafa, Yaser A., Gomaa, Hesham A.M., Youssif, Bahaa G.M., El-Shreef, Essmat M.

“…[Display omitted] •A series of thiazolidine-4-one derivatives as dual EGFR/CDK2 inhibitors has been developed.•Compounds 5d, 5e, and 5f were the most active…”
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Design, Synthesis and Biological Evaluation of New HDAC1 and HDAC2 Inhibitors Endowed with Ligustrazine as a Novel Cap Moiety by Al-Sanea, Mohammad M, Gotina, Lizaveta, Mohamed, Mamdouh Fa, Grace Thomas Parambi, Della, Gomaa, Hesham A M, Mathew, Bijo, Youssif, Bahaa G M, Alharbi, Khalid Saad, Elsayed, Zainab M, Abdelgawad, Mohamed A, Eldehna, Wagdy M

“…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…”
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The Effect of Canertinib on Sensitivity of Cytotoxic Drugs in Tamoxifen-Resistant Breast Cancer Cells In Vitro by Kandeil, M. A., Abdel-Gabbar, Mohamed, Ali, Asmaa T., Gomaa, Hesham A. M.

“…Aims and Objectives. To investigate and examine the reversal effects of canertinib on the activity of EGFR and tamoxifen resistance in drug-resistant human…”
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A comprehensive review of recent advances in the biological activities of quinazolines by Gomaa, Hesham A. M.

“…Quinazoline heterocycles are critical in the development of medications. Quinazoline derivatives have been intensively researched, providing a wide range of…”
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Polymeric Nanoparticles for Delivery of Natural Bioactive Agents: Recent Advances and Challenges by Elmowafy, Mohammed, Shalaby, Khaled, Elkomy, Mohammed H, Alsaidan, Omar Awad, Gomaa, Hesham A M, Abdelgawad, Mohamed A, Mostafa, Ehab M

“…In the last few decades, several natural bioactive agents have been widely utilized in the treatment and prevention of many diseases owing to their unique and…”
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New quinoline/1,2,4-triazole hybrids as dual inhibitors of COX-2/5-LOX and inflammatory cytokines: Design, synthesis, and docking study by Mohassab, Aliaa M., Hassan, Heba A., Abdelhamid, Dalia, Gouda, Ahmed M., Gomaa, Hesham A.M., Youssif, Bahaa G.M., Radwan, Mohamed O., Fujita, Mikako, Otsuka, Masami, Abdel-Aziz, Mohamed

“…•Novel quinoline/1,2,4-triazole hybrids 6a-i and 7a-j as anti-inflammatory agents has been designed and synthesized.•Compounds 6e, 6i, and 7e showed potent…”
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Design and synthesis of new triarylimidazole derivatives as dual inhibitors of BRAFV600E/p38α with potential antiproliferative activity by Youssif, Bahaa G.M., Gouda, Ahmed M., Moustafa, Amr H., Abdelhamid, Antar A., Gomaa, Hesham A.M., Kamal, Islam, Marzouk, Adel A.

“…•A series of novel triaryl-imidazole-based derivatives as dual p38α/ BRAFV600E inhibitors has been designed and synthesized.•Compounds 3b, 3c, 3e, and 3 h were…”
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Design, synthesis, and biological evaluation of new pyrimidine-5-carbonitrile derivatives bearing 1,3-thiazole moiety as novel anti-inflammatory EGFR inhibitors with cardiac safety profile by Abdel-Aziz, Salah A., Taher, Ehab S., Lan, Ping, Asaad, Gihan F., Gomaa, Hesham A.M., El-Koussi, Nawal A., Youssif, Bahaa G.M.

“…[Display omitted] •Novel pyrimidine-5-carbonitrile hybrid with 1,3-thiazole moiety 8a-p as anti-inflammatory EGFR inhibitors has been designed and…”
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Development and assessment of phospholipid-based luteolin-loaded lipid nanocapsules for skin delivery by Elmowafy, Mohammed, Shalaby, Khaled, Elkomy, Mohammed H., Awad Alsaidan, Omar, Gomaa, Hesham A.M., Abdelgawad, Mohamed A., Massoud, Diaa, Salama, Ayman, El-Say, Khalid M.

“…[Display omitted] Luteolin is an excellent flavone possessing several beneficial properties such as antioxidant and anti-inflammatory effects which are…”
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Corrigendum to “Development and assessment of phospholipid-based luteolin-loaded lipid nanocapsules for skin delivery” [Int. J. Pharm. 629 (2022) 122375] by Elmowafy, Mohammed, Shalaby, Khaled, Elkomy, Mohammed H., Alsaidan, Omar Awad, Gomaa, Hesham A.M., Abdelgawad, Mohamed A., Massoud, Diaa, Salama, Ayman, El-Say, Khalid M.

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Design, synthesis, and biological evaluation of novel EGFR inhibitors containing 5-chloro-3-hydroxymethyl-indole-2-carboxamide scaffold with apoptotic antiproliferative activity by Mohamed, Fatma A.M., Gomaa, Hesham A.M., Hendawy, O.M., Ali, Asmaa T., Farghaly, Hatem S., Gouda, Ahmed M., Abdelazeem, Ahmed H., Abdelrahman, Mostafa H., Trembleau, Laurent, Youssif, Bahaa G.M.

“…[Display omitted] •A series of novel indole-2-carboxmide derivatives 9–23 as EGFR inhibitors has been designed and synthesized.•Compounds 10, 11, 13, 15 and…”
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Design, synthesis and antimicrobial activity of novel quinoline-2-one hybrids as promising DNA gyrase and topoisomerase IV inhibitors by Elbastawesy, Mohammed A.I., Mohamed, Fatma A.M., Zaki, Islam, Alahmdi, Mohammed Issa, Alzahrani, Seham S., Alzahrani, Hayat Ali, Gomaa, Hesham A.M., Youssif, Bahaa G.M.

“…•A series of novel quinoline-2-ones/Schiff base hybrids has been designed and synthesized.•The new hybrids were tested against DNA gyrase and topoisomerase IV…”
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Design, synthesis, and antibacterial evaluation of new quinoline-1,3,4-oxadiazole and quinoline-1,2,4-triazole hybrids as potential inhibitors of DNA gyrase and topoisomerase IV by Hofny, Heba A., Mohamed, Mamdouh F.A., Gomaa, Hesham A.M., Abdel-Aziz, Salah A., Youssif, Bahaa G.M., El-koussi, Nawal A., Aboraia, Ahmed S.

“…[Display omitted] •A series of novel quinoline-1,3,4-oxadiazole and quinoline-1,2,4-triazole hybrids has been designed and synthesized.•The new hybrids were…”
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New 1,3,4‐oxadiazoles linked with the 1,2,3‐triazole moiety as antiproliferative agents targeting the EGFR tyrosine kinase by Mahmoud, Mohamed A., Mohammed, Anber F., Salem, Ola I. A., Gomaa, Hesham A. M., Youssif, Bahaa G. M.

“…A series of 1,3,4‐oxadiazole‐1,2,3‐triazole hybrids bearing different pharmacophoric moieties has been designed and synthesized. Their antiproliferative…”
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Optimization and SAR investigation of novel 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivatives as EGFR and BRAFV600E dual inhibitors with potent antiproliferative and antioxidant activities by Gomaa, Hesham A.M., Shaker, Mohamed E., Alzarea, Sami I., Hendawy, O.M., Mohamed, Fatma A.M., Gouda, Ahmed M., Ali, Asmaa T., Morcoss, Martha M., Abdelrahman, Mostafa H., Trembleau, Laurent, Youssif, Bahaa G.M.

“…[Display omitted] •A series of 2,3-dihydropyrazino[1,2-a]indole-1,4-diones 13–22 as dual EGFR/ BRAFV600E inhibitors has been developed.•Compounds 15 and 19–22…”
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Emerging roles of tyrosine kinases in hepatic inflammatory diseases and therapeutic opportunities by Shaker, Mohamed E., Gomaa, Hesham A.M., Abdelgawad, Mohamed A., El-Mesery, Mohamed, Shaaban, Ahmed A., Hazem, Sara H.

“…[Display omitted] •Different tyrosine kinases (TKs) have been implicated in hepatic inflammatory diseases.•A crosstalk is present between TKs and inflammation…”
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