Mitochondria-targeting metallodrugs for cancer therapy: perspectives from cell death modes
ChemMedChem. 2024 May 2:e202400120. doi: 10.1002/cmdc.202400120. Online ahead of print.ABSTRACTMitochondria, recognized as the cellular powerhouses, are indispensable organelles responsible for crucial cellular processes, such as energy metabolism, material synthesis, and signaling transduction. Their intricate involvement in a broad spectrum of diseases, particularly cancer, has propelled the exploration of mitochondria-targeting treatment as a promising strategy for cancer therapy. Since the groundbreaking discovery of cisplatin, the trajectory of research on the development of metal complexes have been marked by continu...
Source: ChemMedChem - May 2, 2024 Category: Chemistry Authors: Zhi Su Hao-Ming Li Meng-Meng Wang Yan Su Hong-Bao Fang Source Type: research
Mitochondria-targeting metallodrugs for cancer therapy: perspectives from cell death modes
ChemMedChem. 2024 May 2:e202400120. doi: 10.1002/cmdc.202400120. Online ahead of print.ABSTRACTMitochondria, recognized as the cellular powerhouses, are indispensable organelles responsible for crucial cellular processes, such as energy metabolism, material synthesis, and signaling transduction. Their intricate involvement in a broad spectrum of diseases, particularly cancer, has propelled the exploration of mitochondria-targeting treatment as a promising strategy for cancer therapy. Since the groundbreaking discovery of cisplatin, the trajectory of research on the development of metal complexes have been marked by continu...
Source: ChemMedChem - May 2, 2024 Category: Chemistry Authors: Zhi Su Hao-Ming Li Meng-Meng Wang Yan Su Hong-Bao Fang Source Type: research
Pd-Catalyzed Coupling of Bromo-N-( β-glucopyranpsyl)quinolin-2-ones with Amides: Synthesis of N-glucosyl-6BrCaQ Conjugates with Potent Anticancer Activity
ChemMedChem. 2024 Apr 30:e202400195. doi: 10.1002/cmdc.202400195. Online ahead of print.ABSTRACTA series of N-glycosyl- 6BrCaQ conjugates was synthesized through a Pd-catalyzed cross-coupling reaction between brominated N-glycosyl quinolin-2-one derivatives and various nitrogen nucleophiles. Antiproliferative assays revealed that this new series of analogues represents a promising class of antitumor compounds as illustrated by the high biological activity observed for several derivatives towards different cancer cell lines compared to the non-glycosylated congeners.PMID:38687188 | DOI:10.1002/cmdc.202400195 (Source: ChemMedChem)
Source: ChemMedChem - April 30, 2024 Category: Chemistry Authors: Wafa Redjdal Sara Benmahdjoub Thi Thanh Hyen Luong Belkacem Benmerad Franck Le Bideau Juliette Vergnaud Samir Messaoudi Source Type: research
Anticonvulsant activity of Tetrahydrolinalool: behavioral, electrophysiological, and molecular docking approaches
In conclusion, all the evidences showed that THL presents effective anticonvulsant activity related to the GABAergic pathway, being a candidate for treatment of epileptic syndromes.PMID:38687623 | DOI:10.1002/cmdc.202400135 (Source: ChemMedChem)
Source: ChemMedChem - April 30, 2024 Category: Chemistry Authors: Diogo V Fons êca Pablo R da Silva Hugo F O Pires Juliana S Rocha Leandra Eug ênia G de Oliveira Flavia M S Reis Erika B M Cavalho Natalia D N Pazos Nat ália F de Sousa Erika C Guedes Leandro R Ribeiro Rita de Cassia S S á Mirian G S S Salvadori Dami à Source Type: research
N-Pyrazolyl- and N-Triazolylamines and -ureas as Antileishmanial and Antitrypanosomal Drugs
ChemMedChem. 2024 Apr 30:e202400220. doi: 10.1002/cmdc.202400220. Online ahead of print.ABSTRACTThree types of modifications of antileishmanial pyrazole lead compounds 7 and 8 were conducted to expand the relationships between structural features and antileishmanial/antitrypanosomal activity: (1) the pyrazole core was retained or replaced by a 1,2,4-triazole ring; (2) various aryl moieties including 2-fluorophenyl, pyridin-3-yl and pyrazin-2-yl rings were attached at 3-position of the core azole; (3) either arylmethylamino or ureido substituents were introduced at 5-position of the azole core. The synthesis followed establ...
Source: ChemMedChem - April 30, 2024 Category: Chemistry Authors: Tobias Winge Lukas Imberg Ben Perry An Matheeusen Guy Caljon Dmitrii Kalinin Bernhard W ünsch Source Type: research
Pd-Catalyzed Coupling of Bromo-N-( β-glucopyranpsyl)quinolin-2-ones with Amides: Synthesis of N-glucosyl-6BrCaQ Conjugates with Potent Anticancer Activity
ChemMedChem. 2024 Apr 30:e202400195. doi: 10.1002/cmdc.202400195. Online ahead of print.ABSTRACTA series of N-glycosyl- 6BrCaQ conjugates was synthesized through a Pd-catalyzed cross-coupling reaction between brominated N-glycosyl quinolin-2-one derivatives and various nitrogen nucleophiles. Antiproliferative assays revealed that this new series of analogues represents a promising class of antitumor compounds as illustrated by the high biological activity observed for several derivatives towards different cancer cell lines compared to the non-glycosylated congeners.PMID:38687188 | DOI:10.1002/cmdc.202400195 (Source: ChemMedChem)
Source: ChemMedChem - April 30, 2024 Category: Chemistry Authors: Wafa Redjdal Sara Benmahdjoub Thi Thanh Hyen Luong Belkacem Benmerad Franck Le Bideau Juliette Vergnaud Samir Messaoudi Source Type: research
Anticonvulsant activity of Tetrahydrolinalool: behavioral, electrophysiological, and molecular docking approaches
In conclusion, all the evidences showed that THL presents effective anticonvulsant activity related to the GABAergic pathway, being a candidate for treatment of epileptic syndromes.PMID:38687623 | DOI:10.1002/cmdc.202400135 (Source: ChemMedChem)
Source: ChemMedChem - April 30, 2024 Category: Chemistry Authors: Diogo V Fons êca Pablo R da Silva Hugo F O Pires Juliana S Rocha Leandra Eug ênia G de Oliveira Flavia M S Reis Erika B M Cavalho Natalia D N Pazos Nat ália F de Sousa Erika C Guedes Leandro R Ribeiro Rita de Cassia S S á Mirian G S S Salvadori Dami à Source Type: research
N-Pyrazolyl- and N-Triazolylamines and -ureas as Antileishmanial and Antitrypanosomal Drugs
ChemMedChem. 2024 Apr 30:e202400220. doi: 10.1002/cmdc.202400220. Online ahead of print.ABSTRACTThree types of modifications of antileishmanial pyrazole lead compounds 7 and 8 were conducted to expand the relationships between structural features and antileishmanial/antitrypanosomal activity: (1) the pyrazole core was retained or replaced by a 1,2,4-triazole ring; (2) various aryl moieties including 2-fluorophenyl, pyridin-3-yl and pyrazin-2-yl rings were attached at 3-position of the core azole; (3) either arylmethylamino or ureido substituents were introduced at 5-position of the azole core. The synthesis followed establ...
Source: ChemMedChem - April 30, 2024 Category: Chemistry Authors: Tobias Winge Lukas Imberg Ben Perry An Matheeusen Guy Caljon Dmitrii Kalinin Bernhard W ünsch Source Type: research
Engineering Cyanine- and Hemicyanine-Based Probes for Optical Imaging of Kidney Diseases
ChemMedChem. 2024 Apr 28:e202400227. doi: 10.1002/cmdc.202400227. Online ahead of print.ABSTRACTMolecular optical probes paly pivotal roles in in vivo imaging of biomarkers associated to kidney diseases. Relying on structural tunability and high fluorescence quantum yields, versatile optical probes have been constructed on cyanine or hemicyanine-based scaffold in recent years. This review summaries the recent progress on the development of optical probes for imaging of kidney diseases, particularly through near-infrared fluorescence, chemiluminescence and photoacoustic imaging modalities. The chemical design and sensing me...
Source: ChemMedChem - April 28, 2024 Category: Chemistry Authors: Shujuan Yi Baoshuai Liang Jiaguo Huang Source Type: research
Sulfonamide bioisosteres of niclosamide enhance antibacterial activity of colistin and bacitracin
ChemMedChem. 2024 Apr 28:e202400175. doi: 10.1002/cmdc.202400175. Online ahead of print.ABSTRACTMulticomponent therapy combining antibiotics with enhancer molecules known as adjuvants is an emerging strategy to combat antimicrobial resistance. Niclosamide is a clinically relevant anthelmintic drug with potential to be repurposed for its inherent antibacterial activity against Gram-positive bacteria and its ability to potentiate the antibacterial activity of colistin against susceptible and resistant Gram-negative bacteria. Herein, sulfonamide analogs of niclosamide were prepared and found to enhance colistin activity again...
Source: ChemMedChem - April 28, 2024 Category: Chemistry Authors: Liam Berry Danyel Ramirez Ronald Domalaon Frank Schweizer Source Type: research
Engineering Cyanine- and Hemicyanine-Based Probes for Optical Imaging of Kidney Diseases
ChemMedChem. 2024 Apr 28:e202400227. doi: 10.1002/cmdc.202400227. Online ahead of print.ABSTRACTMolecular optical probes paly pivotal roles in in vivo imaging of biomarkers associated to kidney diseases. Relying on structural tunability and high fluorescence quantum yields, versatile optical probes have been constructed on cyanine or hemicyanine-based scaffold in recent years. This review summaries the recent progress on the development of optical probes for imaging of kidney diseases, particularly through near-infrared fluorescence, chemiluminescence and photoacoustic imaging modalities. The chemical design and sensing me...
Source: ChemMedChem - April 28, 2024 Category: Chemistry Authors: Shujuan Yi Baoshuai Liang Jiaguo Huang Source Type: research
Sulfonamide bioisosteres of niclosamide enhance antibacterial activity of colistin and bacitracin
ChemMedChem. 2024 Apr 28:e202400175. doi: 10.1002/cmdc.202400175. Online ahead of print.ABSTRACTMulticomponent therapy combining antibiotics with enhancer molecules known as adjuvants is an emerging strategy to combat antimicrobial resistance. Niclosamide is a clinically relevant anthelmintic drug with potential to be repurposed for its inherent antibacterial activity against Gram-positive bacteria and its ability to potentiate the antibacterial activity of colistin against susceptible and resistant Gram-negative bacteria. Herein, sulfonamide analogs of niclosamide were prepared and found to enhance colistin activity again...
Source: ChemMedChem - April 28, 2024 Category: Chemistry Authors: Liam Berry Danyel Ramirez Ronald Domalaon Frank Schweizer Source Type: research
Investigating the serum albumin binding behavior of naphthalimide based fluorophore conjugates: Spectroscopic and molecular docking approach
ChemMedChem. 2024 Apr 27:e202400114. doi: 10.1002/cmdc.202400114. Online ahead of print.ABSTRACTIn the present study, naphthalimide-pyrazole-benzothiazole based fluorescent analogs were synthesized by substituting different primary and secondary amines on the naphthalimide nucleus and were evaluated for their sensitivity and selectivity towards serum albumin. Among various synthesized analogues compound 25 showed the most significant change with serum albumin and was further studied for selective detection and mode of interaction with serum albumin. Here, we compared the binding interaction of fluorescent probe 25 for vari...
Source: ChemMedChem - April 27, 2024 Category: Chemistry Authors: Rohini Gupta Kamaldeep Paul Source Type: research
Investigating the serum albumin binding behavior of naphthalimide based fluorophore conjugates: Spectroscopic and molecular docking approach
ChemMedChem. 2024 Apr 27:e202400114. doi: 10.1002/cmdc.202400114. Online ahead of print.ABSTRACTIn the present study, naphthalimide-pyrazole-benzothiazole based fluorescent analogs were synthesized by substituting different primary and secondary amines on the naphthalimide nucleus and were evaluated for their sensitivity and selectivity towards serum albumin. Among various synthesized analogues compound 25 showed the most significant change with serum albumin and was further studied for selective detection and mode of interaction with serum albumin. Here, we compared the binding interaction of fluorescent probe 25 for vari...
Source: ChemMedChem - April 27, 2024 Category: Chemistry Authors: Rohini Gupta Kamaldeep Paul Source Type: research
Synthesis and Medicinal Applications of N-Heterocyclic Carbene Complexes based on Caffeine and other Xanthines
ChemMedChem. 2024 Apr 26:e202400118. doi: 10.1002/cmdc.202400118. Online ahead of print.ABSTRACTXanthines are purine derivatives predominantly found in plants. These include compounds such as caffeine, theophylline, and theobromine and exhibit a variety of pharmacological properties, demonstrating efficacy in treating neurodegenerative disorders, respiratory dysfunctions, and also in cancer. The versatile attributes of these materials render them privileged scaffolds for the development of compounds for various biological applications. Xanthines are N-heterocyclic carbene precursors that combine a pyrimidine and an imidazo...
Source: ChemMedChem - April 26, 2024 Category: Chemistry Authors: Giulia Francescato Maria In ês Paiva Silva Leitão Giulia Orsini Ana Petronilho Source Type: research
