Design and synthesis of novel imidazole-chalcone derivatives as microtubule protein polymerization inhibitors to treat cervical cancer and reverse cisplatin resistance
Bioorg Chem. 2024 Apr 4;147:107310. doi: 10.1016/j.bioorg.2024.107310. Online ahead of print.ABSTRACTUsing the licochalcone moiety as a lead compound scaffold, 16 novel imidazole-chalcone derivatives were designed and synthesized as microtubule protein polymerization inhibitors. The proliferation inhibitory activities of the derivatives against SiHa (human cervical squamous cell carcinoma), C-33A (human cervical cancer), HeLa (human cervical cancer), HeLa/DDP (cisplatin-resistant human cervical cancer), and H8 (human cervical epithelial immortalized) cells were evaluated. Compound 5a exhibited significant anticancer activi...
Source: Bioorganic Chemistry - April 7, 2024 Category: Chemistry Authors: Zhengye Liu Zheng Yang Mourboul Ablise Source Type: research
Design and synthesis of novel imidazole-chalcone derivatives as microtubule protein polymerization inhibitors to treat cervical cancer and reverse cisplatin resistance
Bioorg Chem. 2024 Apr 4;147:107310. doi: 10.1016/j.bioorg.2024.107310. Online ahead of print.ABSTRACTUsing the licochalcone moiety as a lead compound scaffold, 16 novel imidazole-chalcone derivatives were designed and synthesized as microtubule protein polymerization inhibitors. The proliferation inhibitory activities of the derivatives against SiHa (human cervical squamous cell carcinoma), C-33A (human cervical cancer), HeLa (human cervical cancer), HeLa/DDP (cisplatin-resistant human cervical cancer), and H8 (human cervical epithelial immortalized) cells were evaluated. Compound 5a exhibited significant anticancer activi...
Source: Bioorganic Chemistry - April 7, 2024 Category: Chemistry Authors: Zhengye Liu Zheng Yang Mourboul Ablise Source Type: research
Colchicine for the Prevention of Cardiovascular Disease: Potential Global Implementation
Curr Cardiol Rep. 2024 Apr 4. doi: 10.1007/s11886-024-02049-y. Online ahead of print.ABSTRACTPURPOSE OF REVIEW: Targeting traditional cardiovascular risk factors is effective in reducing recurrent cardiovascular events, yet the presence of residual cardiovascular risk due to underlying systemic inflammation is a largely unaddressed opportunity. This review aims to comprehensively assess the evolving role of colchicine as a therapeutic approach targeting residual inflammatory risk in the context of those with coronary artery disease (CAD).RECENT FINDINGS: Inflammation plays a significant role in promoting atherosclerosis, a...
Source: Atherosclerosis - April 4, 2024 Category: Cardiology Authors: Robert S Zhang Brittany N Weber Diego Araiza-Garaygordobil Michael S Garshick Source Type: research
Colchicine for the Prevention of Cardiovascular Disease: Potential Global Implementation
AbstractPurpose of ReviewTargeting traditional cardiovascular risk factors is effective in reducing recurrent cardiovascular events, yet the presence of residual cardiovascular risk due to underlying systemic inflammation is a largely unaddressed opportunity. This review aims to comprehensively assess the evolving role of colchicine as a therapeutic approach targeting residual inflammatory risk in the context of those with coronary artery disease (CAD).Recent FindingsInflammation plays a significant role in promoting atherosclerosis, and targeting anti-inflammatory pathways has the potential to decrease cardiovascular even...
Source: Current Cardiology Reports - April 4, 2024 Category: Cardiology Source Type: research
An "On Demand" canakinumab regimen for treating children with Colchicine-Resistant familial Mediterranean fever - A multicentre study
CONCLUSION: For individuals with crFMF, COD compared to CFF policy can achieve similar efficacy and safety, with a lower accumulated canakinumab dose, rendering it less immunosuppressive and less expensive.PMID:38569431 | DOI:10.1016/j.intimp.2024.111967 (Source: International Immunopharmacology)
Source: International Immunopharmacology - April 3, 2024 Category: Allergy & Immunology Authors: Katy Shehadeh Yoel Levinsky Shelly Kagan Tarek Zuabi Rotem Tal Neta Hana Aviran Yonatan Butbul Aviel Irit Tirosh Shiri Spielman Adi Miller-Barmak Rotem Semo Oz Liora Harel Gabriel Chodick Gil Amarilyo Source Type: research
Tobacco smoke condensate-induced senescence in endothelial cells was ameliorated by colchicine treatment via suppression of NF- κB and MAPKs P38 and ERK pathways activation
Smoking is the major cause of cardiovascular diseases and cancer. It induces oxidative stress, leading to DNA damage and cellular senescence. Senescent cells increase the expression and release of pro-inflamma... (Source: Cell Communication and Signaling)
Source: Cell Communication and Signaling - April 3, 2024 Category: Molecular Biology Authors: Dilaware Khan, Huakang Zhou, Jinliang You, Vera Annika Kaiser, Rajiv K Khajuria and Sajjad Muhammad Tags: Research Source Type: research
Prednisolone Versus Colchicine for Acute Gout in Primary Care: statistical analysis plan for the pragmatic, multicenter, randomized, and double-blinded COPAGO non-inferiority trial
To date, colchicine and prednisolone are two effective therapies for the treatment of acute gout but have never been compared directly in a randomized clinical trial. In addition, in previous trials of treatin... (Source: Trials)
Source: Trials - April 3, 2024 Category: General Medicine Authors: Adrian Richter, Julia Truthmann, Eva Hummers, Julia Freyer Martins Pereira, Ildik ó Gágyor, Franziska Schuster, Amelie Witte, Susanne Böhm, Alexandra Greser, Petra Kamin, Sylvia Stracke, Marcus Dörr, Robin Bülow, Stefan Engeli, Jean François Chenot Tags: Update Source Type: research
High systemic inflammation as a novel cardiovascular risk factor and target for anti-cytokine therapy: comment regarding the triglyceride glucose index
Int J Cardiovasc Imaging. 2024 Apr 1. doi: 10.1007/s10554-024-03046-6. Online ahead of print.ABSTRACTIn the last century, there has been more than enough research that proved the association of high lipid and glucose levels with cardiovascular disease, thus establishing the current well-known traditional cardiovascular risk factors such as dyslipidemia, diabetes, and metabolic syndrome. Hence, these cardiovascular risk factors are target therapy for glucose and lipid-lowering agents to prevent adverse cardiovascular events. However, despite controlling the lipid and glucose levels, some studies demonstrated the subclinical...
Source: Atherosclerosis - April 1, 2024 Category: Cardiology Authors: Artemio Garc ía-Escobar Rosa L ázaro-García Jos é-Ángel Cabrera Alfonso Jurado-Rom án Ra úl Moreno Source Type: research
High systemic inflammation as a novel cardiovascular risk factor and target for anti-cytokine therapy: comment regarding the triglyceride glucose index
AbstractIn the last century, there has been more than enough research that proved the association of high lipid and glucose levels with cardiovascular disease, thus establishing the current well-known traditional cardiovascular risk factors such as dyslipidemia, diabetes, and metabolic syndrome. Hence, these cardiovascular risk factors are target therapy for glucose and lipid-lowering agents to prevent adverse cardiovascular events. However, despite controlling the lipid and glucose levels, some studies demonstrated the subclinical atherosclerosis suggesting that these cardiovascular risk factors alone cannot account for t...
Source: The International Journal of Cardiovascular Imaging - April 1, 2024 Category: Radiology Source Type: research
Design, synthesis and biological evaluation of new 2,6-difluorinated phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new antimicrotubule agents
In this study, we evaluated the effect of the difluorination of the aromatic ring bearing the imidazolidin-2-one moiety (ring A) at positions 3, 5 and 2, 6 on their antiproliferative activity on four cancer cell lines, their ability to disrupt the microtubules and their toxicity toward chick embryos. We thus synthesized, characterized and biologically evaluated 24 new difluorinated PIB-SO derivatives designated as phenyl 3,5-difluoro-4-(2-oxoimidazolidin-1-yl)benzenesulfonates (3,5-PFB-SOs, 4-15) and phenyl 2,6-difluoro-4-(2-oxoimidazolidin-1-yl)benzenesulfonates (2,6-PFB-SOs, 16-27). The concentration of the drug required...
Source: Bioorganic Chemistry - March 28, 2024 Category: Chemistry Authors: Chahrazed Bouzriba Mathieu Gagn é-Boulet Atziri Corin Chavez Alvarez Vincent Ouellette Isabelle Laverdi ère S ébastien Fortin Source Type: research
Design, synthesis and biological evaluation of new 2,6-difluorinated phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new antimicrotubule agents
In this study, we evaluated the effect of the difluorination of the aromatic ring bearing the imidazolidin-2-one moiety (ring A) at positions 3, 5 and 2, 6 on their antiproliferative activity on four cancer cell lines, their ability to disrupt the microtubules and their toxicity toward chick embryos. We thus synthesized, characterized and biologically evaluated 24 new difluorinated PIB-SO derivatives designated as phenyl 3,5-difluoro-4-(2-oxoimidazolidin-1-yl)benzenesulfonates (3,5-PFB-SOs, 4-15) and phenyl 2,6-difluoro-4-(2-oxoimidazolidin-1-yl)benzenesulfonates (2,6-PFB-SOs, 16-27). The concentration of the drug required...
Source: Bioorganic Chemistry - March 28, 2024 Category: Chemistry Authors: Chahrazed Bouzriba Mathieu Gagn é-Boulet Atziri Corin Chavez Alvarez Vincent Ouellette Isabelle Laverdi ère S ébastien Fortin Source Type: research
Correction: Separable and Inseparable Silk Fibroin Microneedles for the Transdermal Delivery of Colchicine: Development, Characterization, and Comparisons
AAPS PharmSciTech. 2024 Mar 22;25(4):65. doi: 10.1208/s12249-024-02779-w.NO ABSTRACTPMID:38519629 | DOI:10.1208/s12249-024-02779-w (Source: AAPS PharmSciTech)
Source: AAPS PharmSciTech - March 23, 2024 Category: Drugs & Pharmacology Authors: Shiji Liao Guirong Qiu Yanping Hu Bohong Guo Yuqin Qiu Source Type: research
Correction: Separable and Inseparable Silk Fibroin Microneedles for the Transdermal Delivery of Colchicine: Development, Characterization, and Comparisons
AAPS PharmSciTech. 2024 Mar 22;25(4):65. doi: 10.1208/s12249-024-02779-w.NO ABSTRACTPMID:38519629 | DOI:10.1208/s12249-024-02779-w (Source: AAPS PharmSciTech)
Source: AAPS PharmSciTech - March 23, 2024 Category: Drugs & Pharmacology Authors: Shiji Liao Guirong Qiu Yanping Hu Bohong Guo Yuqin Qiu Source Type: research
Correction: Separable and Inseparable Silk Fibroin Microneedles for the Transdermal Delivery of Colchicine: Development, Characterization, and Comparisons
AAPS PharmSciTech. 2024 Mar 22;25(4):65. doi: 10.1208/s12249-024-02779-w.NO ABSTRACTPMID:38519629 | DOI:10.1208/s12249-024-02779-w (Source: AAPS PharmSciTech)
Source: AAPS PharmSciTech - March 23, 2024 Category: Drugs & Pharmacology Authors: Shiji Liao Guirong Qiu Yanping Hu Bohong Guo Yuqin Qiu Source Type: research
Correction: Separable and Inseparable Silk Fibroin Microneedles for the Transdermal Delivery of Colchicine: Development, Characterization, and Comparisons
AAPS PharmSciTech. 2024 Mar 22;25(4):65. doi: 10.1208/s12249-024-02779-w.NO ABSTRACTPMID:38519629 | DOI:10.1208/s12249-024-02779-w (Source: AAPS PharmSciTech)
Source: AAPS PharmSciTech - March 23, 2024 Category: Drugs & Pharmacology Authors: Shiji Liao Guirong Qiu Yanping Hu Bohong Guo Yuqin Qiu Source Type: research
