Enaminone-based carboxylic acids as novel non-classical carbonic anhydrases inhibitors: design, synthesis and in vitro biological assessment

Autor: Mahmoud F. Abo-Ashour, Hadia Almahli, Alessandro Bonardia, Amira Khalil, Tarfah Al-Warhi, Sara T. Al-Rashood, Hatem A. Abdel-Aziz, Alessio Nocentini, Claudiu T. Supuran, Wagdy M. Eldehna

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 37, Iss 1, Pp 2256-2264 (2022)

In searching for new molecular drug targets, Carbonic Anhydrases (CAs) have emerged as valuable targets in diverse diseases. CAs play critical functions in maintaining pH and CO2 homeostasis, metabolic pathways, and much more. So, it is becoming attr

Externí odkaz: https://doaj.org/article/36287e74dd30418bb742055917f5a846

Development of 2-oxindolin-3-ylidene-indole-3-carbohydrazide derivatives as novel apoptotic and anti-proliferative agents towards colorectal cancer cells

Autor: Wagdy M. Eldehna, Mahmoud F. Abo-Ashour, Tarfah Al-Warhi, Sara T. Al-Rashood, Amal Alharbi, Rezk R. Ayyad, Khayal Al-Khayal, Maha Abdulla, Hatem A. Abdel-Aziz, Rehan Ahmad, Radwan El-Haggar

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 36, Iss 1, Pp 320-329 (2021)

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 such proteins has become a validated and attractive t

Externí odkaz: https://doaj.org/article/ae0ff9bf7af7424389e31b9650cd019c

Novel [(3-indolylmethylene)hydrazono]indolin-2-ones as apoptotic anti-proliferative agents: design, synthesis and in vitro biological evaluation

Autor: Wagdy M. Eldehna, Mahmoud F. Abo-Ashour, Hany S. Ibrahim, Ghada H. Al-Ansary, Hazem A. Ghabbour, Mahmoud M. Elaasser, Hanaa Y. A. Ahmed, Nesreen A. Safwat

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 33, Iss 1, Pp 686-700 (2018)

On account of their significance as apoptosis inducing agents, merging indole and 3-hydrazinoindolin-2-one scaffolds is a logic tactic for designing pro-apoptotic agents. Consequently, 27 hybrids (6a–r, 9a–f and 11a–c) were synthesised and eval

Externí odkaz: https://doaj.org/article/d5ad79c0e553437ca23de71e8a6713c4

Novel [(N-alkyl-3-indolylmethylene)hydrazono]oxindoles arrest cell cycle and induce cell apoptosis by inhibiting CDK2 and Bcl-2: synthesis, biological evaluation and in silico studies

Autor: Mohammad M. Al-Sanea, Wagdy M. Eldehna, Ghada H. Al-Ansary, Hatem A. Abdel-Aziz, Mahmoud F. Abo-Ashour, Hanaa Y. Ahmed, Tarfah Al-Warhi, Hadia Almahli, Mahmoud M. Elaasser, Ohoud J. Alotaibi

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 35, Iss 1, Pp 1300-1309 (2020)
Journal of Enzyme Inhibition and Medicinal Chemistry
article-version (VoR) Version of Record

As a continuation for our previous work, a novel set of N-alkylindole-isatin conjugates (7, 8a–c, 9 and 10a–e) is here designed and synthesised with the prime aim to develop more efficient isatin-based antitumor candidates. Utilising the SAR outp

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c72d7334888e7f8968b51b5691b79d4d
https://doaj.org/article/a7e62eb9296f40d3b752213c6be30565

Novel synthesized SLC-0111 thiazole and thiadiazole analogues: Determination of their carbonic anhydrase inhibitory activity and molecular modeling studies

Autor: Silvia Bua, Mahmoud F. Abo-Ashour, Claudiu T. Supuran, Hatem A. Abdel-Aziz, Sahar M. Abou-Seri, Wagdy M. Eldehna, Alessio Nocentini, Hany S. Ibrahim

Publikováno v: Bioorganic Chemistry. 87:794-802

In the presented work, we report the design and synthesis of novel SLC-0111 thiazole and thiadiazole analogues (11a–d, 12a–d, 16a–c and 17a–d). A bioisosteric replacement approach was adopted to replace the 4-fluorophenyl tail of SLC-0111 wit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aa73ad11163772331ad10466633065b1
https://doi.org/10.1016/j.bioorg.2019.04.002