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Search Results (4)

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Keywords = benzodiazepinones

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16 pages, 1054 KiB  
Article
New Class of Benzodiazepinone Derivatives as Pro-Death Agents Targeting BIR Domains in Cancer Cells
by Michele Fiore, Michele Mosconi, Francesco Bonì, Alice Parodi, Annalisa Salis, Bruno Tasso, Eloise Mastrangelo, Enrico Millo and Federica Cossu
Molecules 2023, 28(1), 446; https://doi.org/10.3390/molecules28010446 - 3 Jan 2023
Viewed by 3161
Abstract
Inhibitor of Apoptosis Proteins (IAPs) are validated targets for cancer therapy, and the deregulation of their activities within the NF-κB pathway correlates with chemoresistance events, even after treatment with IAPs-antagonists in the clinic (Smac-mimetics). The molecule FC2 was identified as a NF-κB pathway [...] Read more.
Inhibitor of Apoptosis Proteins (IAPs) are validated targets for cancer therapy, and the deregulation of their activities within the NF-κB pathway correlates with chemoresistance events, even after treatment with IAPs-antagonists in the clinic (Smac-mimetics). The molecule FC2 was identified as a NF-κB pathway modulator in MDA-MB-231 adenocarcinoma cancer cells after virtual screening of the Chembridge library against the Baculoviral IAP Repeat 1 (BIR1) domain of cIAP2 and XIAP. An improved cytotoxic effect is observed when FC2 is combined with Smac-mimetics or with the cytokine Tumor Necrosis Factor (TNF). Here, we propose a library of 22 derivatives of FC2, whose scaffold was rationally modified starting from the position identified as R1. The cytotoxic effect of FC2 derivatives was evaluated in MDA-MB-231 and binding to the cIAP2- and XIAP-BIR1 domains was assessed in fluorescence-based techniques and virtual docking. Among 22 derivatives, 4m and 4p display improved efficacy/potency in MDA-MB-231 cells and low micromolar binding affinity vs the target proteins. Two additional candidates (4b and 4u) display promising cytotoxic effects in combination with TNF, suggesting the connection between this class of molecules and the NF-κB pathway. These results provide the rationale for further FC2 modifications and the design of novel IAP-targeting candidates supporting known therapies. Full article
(This article belongs to the Special Issue Anticancer Compounds with Different Biological Targets)
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17 pages, 2034 KiB  
Article
Regioselective One-Pot Synthesis, Biological Activity and Molecular Docking Studies of Novel Conjugates N-(p-Aryltriazolyl)-1,5-benzodiazepin-2-ones as Potent Antibacterial and Antifungal Agents
by Asma Nsira, Hasan Mtiraoui, Sami Chniti, Hanan Al-Ghulikah, Rafik Gharbi and Moncef Msaddek
Molecules 2022, 27(13), 4015; https://doi.org/10.3390/molecules27134015 - 22 Jun 2022
Cited by 8 | Viewed by 2083
Abstract
Novel 1,2,3-triazolo-linked-1,5-benzodiazepinones were designed and synthesized via a Cu(I)-catalyzed 1,3-dipolar alkyne-azide coupling reaction (CuAAC). The chemical structures of these compounds were confirmed by 1H NMR, 13C NMR, HMBC, HRMS, and elemental analysis. The compounds were screened for their in vitro antibacterial [...] Read more.
Novel 1,2,3-triazolo-linked-1,5-benzodiazepinones were designed and synthesized via a Cu(I)-catalyzed 1,3-dipolar alkyne-azide coupling reaction (CuAAC). The chemical structures of these compounds were confirmed by 1H NMR, 13C NMR, HMBC, HRMS, and elemental analysis. The compounds were screened for their in vitro antibacterial and antifungal activities. Several compounds exhibited good to moderate activities compared to those of established standard drugs. Furthermore, the binding interactions of these active analogs were confirmed through molecular docking. Full article
(This article belongs to the Special Issue Click Chemistry in Organic Synthesis)
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2 pages, 100 KiB  
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(4Z)-1-Benzyl (1,3-Dibenzyl)-4-(2-oxopropylidene)-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one
by Ould Mohamed Sidya Mohamed Said, Bouhfid Rachid, Nicolas Joly, Vincent Lequart, Patrick Martin, M. Massoui and El Mokhtar Essassi
Molbank 2006, 2006(5), M499; https://doi.org/10.3390/M499 - 1 Sep 2006
Viewed by 4770
Abstract
We describe in this work the synthesis of new benzodiazepine derivatives susceptible to possess various pharmacological activities.[...] Full article
3 pages, 111 KiB  
Short Note
(4Z)-1-Propargyl(1,3-Dipropargyl)-4-(2-oxopropylidene)-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one
by Ould Mohamed Sidya Mohamed Said, Bouhfid Rachid, Nicolas Joly, Vincent Lequart, Patrick Martin, M. Massoui and El Mokhtar Essassi
Molbank 2006, 2006(5), M498; https://doi.org/10.3390/M498 - 1 Sep 2006
Viewed by 4833
Abstract
We describe in this work the synthesis of new benzodiazepine derivatives susceptible to possess various pharmacological activities.[...] Full article
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