Synthesis, Biological Evaluation, and Docking Studies of Pyrazole-Linked Benzothiazole Hybrids as Promising Anti-Tb Agents

Autor: Reham A. Mohamed-Ezzat, Mohamed A. Omar, Ahmed Temirak, Ahmed S. Abdelsamie, Marwa M. Abdel-Aziz, Shadia A. Galal, galal elgemeie, Hoda I. El Diwani, Keith J. Flanagan, Mathias O. Senge

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ef70908f8b2acc332bf80588689259fa
https://doi.org/10.2139/ssrn.4446503

Dual Targeting of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 by a Novel Drug-Prodrug Approach: A Potential Therapeutic Option for the Treatment of Endometriosis

Autor: Abdelrahman Mohamed, Mohamed Salah, Mariam Tahoun, Manuel Hawner, Ahmed S. Abdelsamie, Martin Frotscher

Publikováno v: Journal of medicinal chemistry. 65(17)

A novel approach for the dual inhibition of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1(17β HSD1) by a single drug was explored, starting from in-house 17β HSD1 inhibitors via masking their phenolic OH group with a sulfamat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::16cdeffc24d89f049400a1ed565610da
https://pubmed.ncbi.nlm.nih.gov/35993890

17β-Hydroxysteroid Dehydrogenase Type 1 Inhibition: A Potential Treatment Option for Non-Small Cell Lung Cancer

Autor: Rolf W. Hartmann, Chris J. van Koppen, Matthias W. Laschke, Giuseppe Felice Mangiatordi, Ahmed S. Abdelsamie, Martin Frotscher, Orazio Nicolotti, Abdelrahman Mohamed, Angelo Carotti, Arcangela Mazzini, Hanna Drzewiecka, Emanuele M. Gargano, Paweł P. Jagodziński, Sandrine Marchais-Oberwinkler

Publikováno v: ACS medicinal chemistry letters
United States
ACS Med Chem Lett
ACS medicinal chemistry letters (2021). doi:10.1021/acsmedchemlett.1c00462
info:cnr-pdr/source/autori:Emanuele M. Gargano, Abdelrahman Mohamed, Ahmed S. Abdelsamie, Giuseppe F. Mangiatordi, Hanna Drzewiecka, Pawe? P. Jagodzi?ski, Arcangela Mazzini, Chris J. van Koppen, Matthias W. Laschke, Orazio Nicolotti, Angelo Carotti, Sandrine Marchais-Oberwinkler, Rolf W. Hartmann, and Martin Frotscher/titolo:17?-Hydroxysteroid Dehydrogenase Type 1 Inhibition: A Potential Treatment Option for Non-Small Cell Lung Cancer/doi:10.1021%2Facsmedchemlett.1c00462/rivista:ACS medicinal chemistry letters/anno:2021/pagina_da:/pagina_a:/intervallo_pagine:/volume

[Image: see text] In the face of the clinical challenge posed by non-small cell lung cancer (NSCLC), the present need for new therapeutic approaches is genuine. Up to now, no proof existed that 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) is

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4b72b1eb9a0d3948ea61df325c6e341e
https://hdl.handle.net/10033/623149

Divergent synthesis and biological evaluation of 2-(trifluoromethyl)pyridines as virulence-attenuating inverse agonists targeting PqsR

Autor: Andreas M. Kany, Teresa Röhrig, Wulf Blankenfeldt, Maximilian Bauer, Andrea Scrima, Mostafa M. Hamed, Christian Schütz, Stefan Schmelz, Amir Hodzic, Ahmed S. Abdelsamie, Martin Empting

Publikováno v: European journal of medicinal chemistry. 226

A short and divergent route towards new derivatives of 2-(trifluoromethyl)pyridines as potent inverse agonists of the bacterial target PqsR against Pseudomonas aeruginosa (PA) infections is described. This Gram-negative pathogen causes severe nosocom

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5607c322d962904fb92bbdba8653a811
https://pubmed.ncbi.nlm.nih.gov/34520957

Part I: Design, synthesis and biological evaluation of novel pyrazole-benzimidazole conjugates as checkpoint kinase 2 (Chk2) inhibitors with studying their activities alone and in combination with genotoxic drugs

Autor: Mamdouh M. Ali, Reem El-Shenawy, Ahmed S. Abdelsamie, Samia A. Shouman, H. I. El-Diwani, Adel S. Girgis, Shadia A. Galal, Hamed I. Ali, Abeer H. Abdel-Halim, Yasmine S El Abd, Abeer E. Mahmoud, Ashraf A Tabll, Yasmin M. Attia, Amal A. Fyiad

Publikováno v: European Journal of Medicinal Chemistry. 134:392-405

Activated checkpoint kinase 2 (Chk2) is a tumor suppressor as one of the main enzymes that affect the cell cycle. 2-Biarylbenzimidazoles are potent selective class of Chk2 inhibitors; the structure-based design was applied to synthesize a new series

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1003125a65d3000560ee9f8cdb184a70
https://doi.org/10.1016/j.ejmech.2017.03.090