Article
Biochemistry & Molecular Biology
Diana R. Melis, Chiao-Yu Hsiao, Jill M. Combrinck, Lubbe Wiesner, Gregory S. Smith
Summary: The fluorescent analogue of a previously synthesised N,N-chelated Ir-III complex displayed micromolar activity against the chloroquine-sensitive NF54 strain of Plasmodium falciparum, without interfering with DNA replication. The fluorescence saturation near phospholipid structures suggests an essential association with membranes or organelles for the efficacy of these antimalarial compounds.
Article
Chemistry, Inorganic & Nuclear
Nadia Baartzes, Jill Combrinck, Kelly Chibale, Gregory S. Smith
Summary: In this study, a series of cationic Rh(III) polypyridyl aminoquinoline-benzimidazole hybrid complexes were synthesized and evaluated for their in vitro antiplasmodial activity. The hybrid complexes showed good activity against the chloroquine-sensitive strain of Plasmodium falciparum and maintained activity against the multidrug-resistant strain, with low to no cytotoxicity. Selected active hybrid complexes also demonstrated significant inhibition of beta-haematin formation.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Yong Wang, Pascal Pigeon, Wei Li, Jiangkun Yan, Patrick M. Dansette, Mohamed Othman, Michael J. McGlinchey, Gerard Jaouen
Summary: Ferrociphenols, compounds characterized by a biologically active redox motif, have anticancer properties. This study synthesized a variety of ferrociphenols with nitrogen-containing substituents and investigated their structure-activity relationships. Oxidative metabolism experiments and ROS-related bioactivity measurements were conducted to explore the cytotoxicity of imidoferrociphenols. Additionally, dimerization phenomenon observed in the crystal structure of a ferrociphenol may affect its antitumor activity.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Alice De Palo, Dijana Draca, Maria Grazia Murrali, Stefano Zacchini, Guido Pampaloni, Sanja Mijatovic, Danijela Maksimovic-Ivanic, Fabio Marchetti
Summary: Piano-stool iridium complexes based on the pentamethylcyclopentadienyl ligand have been extensively studied as potential anticancer drugs, with two complexes showing significant antiproliferative activity on multiple cancer cell lines. These complexes do not affect the viability of primary mouse peritoneal cells and exert their tumoricidal effects through a combination of effects on cellular proliferation, apoptosis, and senescence triggered by mitochondrial failure and reactive oxygen and nitrogen species production.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Mziyanda Mbaba, Laura M. K. Dingle, Ayanda I. Zulu, Dustin Laming, Tarryn Swart, Jo-Anne de la Mare, Heinrich C. Hoppe, Adrienne L. Edkins, Setshaba D. Khanye
Summary: A series of tailored coumarin-based ferrocenyl 1,3-oxazine hybrid compounds were synthesized and found to exhibit higher in vitro antiparasitic potency against malaria and trypanosomiasis. Structure-activity relationship analyses suggest that the presence of the coumarin nucleus is tolerated for biological activity but may lead to reduced efficacy. Preliminary mechanistic studies with the most promising compound support hemozoin inhibition and DNA interaction as potential mechanisms for producing plasmocidal and antitrypanosomal effects.
Article
Biochemistry & Molecular Biology
Fatima-Zahra Ishmail, Diana R. Melis, Mziyanda Mbaba, Gregory S. Smith
Summary: A diverse series of tricarbonyl manganese and rhenium complexes linked to a quinoline-triazole hybrid scaffold were synthesized and their inhibitory activities against Plasmodium falciparum were evaluated. The complexes exhibited moderate activity, with the photoactivatable manganese(I) tricarbonyl complexes showing enhanced inhibitory activities against the malaria parasite. Additionally, the complexes retained their activity in multidrug-resistant strains of Plasmodium falciparum, suggesting a potential novel route for designing antimalarial agents with higher efficacy.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Francis Kayamba, Mbuso Faya, Ofentse Jacob Pooe, Babita Kushwaha, Narva Deshwar Kushwaha, Vincent A. Obakachi, Vincent O. Nyamori, Rajshekhar Karpoormath
Summary: This review highlights the importance of parasitic lactate dehydrogenases (LDH) and malate dehydrogenases (MDH) as potential therapeutic targets for the development of novel antiparasitic agents. These enzymes play a critical role in the progression and development of parasitic diseases, making them essential for the future development of effective treatments.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Inorganic & Nuclear
Janina Schmidt, Jessica Woelker, Petra Lippmann, Ingo Ott
Summary: Organometallic rhodium(I) complexes were synthesized and evaluated for their cytotoxic effects against cancer cells. The complexes exhibited strong cytotoxic effects on various cancer cell lines, with a preference for branched isopropyl side chains on the N-heterocyclic carbene ligands. Further studies suggested that the increased cytotoxicity might be attributed to higher cellular uptake.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Nanang Rudianto Ariefta, Baldorj Pagmadulam, Coh-ichi Nihei, Yoshifumi Nishikawa
Summary: This study evaluated the growth-inhibitory effects of the antimalarial agent sparsomycin against drug-resistant malaria parasites. The results showed that sparsomycin had inhibitory effects on both sensitive and resistant strains of the parasites. This study suggests that sparsomycin has potential as an alternative treatment for malaria.
Review
Chemistry, Medicinal
Sergio Wittlin, Pascal Maeser
Summary: The specificity of drug action is based on the concept of drug targets, looking for proteins that are essential for the pathogen but not present in human cells. Some drugs can selectively kill pathogens by activating prodrugs inside the pathogen while remaining inactive in the host.
ACS INFECTIOUS DISEASES
(2021)
Article
Parasitology
Natali de Franca Nibbering Santos, Natanael da Silva Bezerra Jr, Jamerson Ferreira de Oliveira, Denise Maria Figueiredo Araujo Duarte, Jose Cleberson dos Santos Soares, Diego Santa Clara Marques, Aline Caroline da Silva Santos, Fatima Nogueira, Valeria Rego Alves Pereira, Maria Carmo Alves de Lima, Iranildo Jose da Cruz Filho
Summary: In this study, 13 thiosemicarbazones and 16 thiazoles were synthesized and characterized. The pharmacokinetic properties of these compounds showed good bioavailability and permeability. Thiosemicarbazones exhibited moderate to high antioxidant potential and could interact with albumin and DNA. They also showed lower toxicity to mammalian cells compared to thiazoles. Both thiosemicarbazones and thiazoles exhibited cytotoxic potential against Leishmania amazonensis and Trypanosoma cruzi parasites. However, thiosemicarbazones did not inhibit the growth of Plasmodium falciparum, while thiazoles showed growth inhibition. This study suggests that the synthesized compounds have in vitro antiparasitic potential.
EXPERIMENTAL PARASITOLOGY
(2023)
Article
Chemistry, Medicinal
Theresa Hermann, Robin Wallner, Johanna Dolensky, Werner Seebacher, Eva-Maria Pferschy-Wenzig, Marcel Kaiser, Pascal Maser, Robert Weis
Summary: The compound MMV030666 in MMV's Malaria Box exhibits multi-stage activity against various strains of Plasmodium falciparum without resistance development. By modifying the structure, a series of compounds were prepared and the relationship between the structure and activity was revealed. Furthermore, the pharmacokinetic and physicochemical parameters were improved.
Article
Biochemistry & Molecular Biology
Anna Jaromin, Anna Czopek, Silvia Parapini, Nicoletta Basilico, Ernest Misiak, Jerzy Gubernator, Agnieszka Zagorska
Summary: This study synthesized novel derivatives and conducted preliminary physicochemical characterization, showing strong inhibitory effects against Plasmodium falciparum, particularly the chloroquine-resistant strain. These molecules exhibited no hemolytic action on human erythrocytes and low toxicity on mammalian cell line.
Article
Chemistry, Inorganic & Nuclear
Juan Sanz Garcia, Marie Gaschard, Isabelle Navizet, Mehdi Sahihi, Siden Top, Yong Wang, Pascal Pigeon, Anne Vessieres, Michele Salmain, Gerard Jaouen
Summary: The family of ferrocifens, derived from the anti-oestrogen tamoxifen, exhibit a broad antitumor activity by generating reactive oxygen species and electrophilic quinone methides. In addition to their known targets, cathepsin B was unexpectedly identified as a new target for ferrocifens.
EUROPEAN JOURNAL OF INORGANIC CHEMISTRY
(2022)
Article
Microbiology
Nanang R. Ariefta, Baldorj Pagmadulam, Masaki Hatano, Noriko Ikeda, Kunio Isshiki, Kazuaki Matoba, Masayuki Igarashi, Coh-ichi Nihei, Yoshifumi Nishikawa
Summary: The increasing burden and spread of resistant malaria parasites have driven the demand for a new therapeutic agent. Phebestin showed nanomolar efficacy against Plasmodium falciparum 3D7 and inhibited parasite multiplication in vitro. It exhibited no cytotoxicity against human cells and inhibited parasite stages at high concentrations. In vivo evaluation in mice infected with different malaria strains also showed promising results.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2023)
Article
Biochemistry & Molecular Biology
Diana R. Melis, Chiao-Yu Hsiao, Jill M. Combrinck, Lubbe Wiesner, Gregory S. Smith
Summary: The fluorescent analogue of a previously synthesised N,N-chelated Ir-III complex displayed micromolar activity against the chloroquine-sensitive NF54 strain of Plasmodium falciparum, without interfering with DNA replication. The fluorescence saturation near phospholipid structures suggests an essential association with membranes or organelles for the efficacy of these antimalarial compounds.
Article
Chemistry, Inorganic & Nuclear
Timothy J. Kotze, Sandra Duffy, Vicky M. Avery, Audrey Jordaan, Digby F. Warner, Leigh Loots, Gregory S. Smith, Prinessa Chellan
Summary: Six new iridium complexes with amidosulfadoxine ligands were synthesized and tested for inhibitory activities against Plasmodium falciparum and Mycobacterium tuberculosis. One complex, C6, exhibited potent activity against Pf 3D7 and the multidrug-resistant Pf Dd2 strains, showing promising potential for further development as antimalarial drugs.
INORGANICA CHIMICA ACTA
(2021)
Article
Biochemistry & Molecular Biology
Fatima-Zahra Ishmail, Diana R. Melis, Mziyanda Mbaba, Gregory S. Smith
Summary: A diverse series of tricarbonyl manganese and rhenium complexes linked to a quinoline-triazole hybrid scaffold were synthesized and their inhibitory activities against Plasmodium falciparum were evaluated. The complexes exhibited moderate activity, with the photoactivatable manganese(I) tricarbonyl complexes showing enhanced inhibitory activities against the malaria parasite. Additionally, the complexes retained their activity in multidrug-resistant strains of Plasmodium falciparum, suggesting a potential novel route for designing antimalarial agents with higher efficacy.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2021)
Article
Chemistry, Inorganic & Nuclear
Nikechukwu N. Omosun, Gregory S. Smith
Summary: The synthesis of two water-soluble Rh(I) complexes and their performance as catalyst precursors in aqueous biphasic hydroformylation reaction were reported. Both catalyst precursors showed high activity and good selectivity, but experienced a decrease in conversion after multiple cycles.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2021)
Article
Chemistry, Inorganic & Nuclear
Nozuko M. Motimani, Siyabonga Ngubane, Gregory S. Smith
Summary: Polynuclear heteroleptic ruthenium(II) photosensitizers combining imine or amine-functionalised bipyridyl ligands were synthesized and investigated for their photoreactivity. The complexes showed red-shifted emission spectra and exhibited high yields as visible-light photoredox catalysts in the hydrothiolation reaction of olefins.
Article
Biochemistry & Molecular Biology
Aleksandra Kowalczyk, Michal Piotrowicz, Magdalena Gapinska, Damian Trzybinski, Krzysztof Wozniak, Taryn M. Golding, Tameryn Stringer, Gregory S. Smith, Rafal Czerwieniec, Konrad Kowalski
Summary: The knowledge regarding the chemistry and biological activity of glycol nucleic acid (GNA) components is limited. The synthesized phenanthrenyl GNA nucleoside and gemcitabine exhibit similar mechanisms of anticancer activity in HeLa cancer cells. Additionally, these compounds also show some activity in antiplasmodial assays.
BIOORGANIC CHEMISTRY
(2022)
Article
Chemistry, Inorganic & Nuclear
Nosipho Msimango, Athi Welsh, Sharon Prince, Gregory S. Smith
Summary: This article describes the synthesis, characterization, and cytotoxicity of a novel tris-benzimidazole-quinoline hybrid ligand and its corresponding cationic trimetallic complexes. The complexes show stability in DMSO and exhibit antiproliferative properties against human breast cancer cells, with the ruthenium(II) p-cymene complex being the most active.
INORGANIC CHEMISTRY COMMUNICATIONS
(2022)
Article
Biochemistry & Molecular Biology
Sara Nasiri Sovari, Taryn M. Golding, Mziyanda Mbaba, Roxanne Mohunlal, Timothy J. Egan, Gregory S. Smith, Fabio Zobi
Summary: A small library of aminoquinoline and imidazolopiperidine (IMP)-based ligands showed potent inhibitory activities against chloroquine-sensitive (CQS) and multidrug-resistant (MDR) strains of P. falciparum. The compounds may act through hemozoin inhibition and the quinoline-based compounds exhibited higher binding affinities than the reference drug chloroquine.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2022)
Article
Chemistry, Inorganic & Nuclear
Nadia Baartzes, Jill Combrinck, Kelly Chibale, Gregory S. Smith
Summary: In this study, a series of cationic Rh(III) polypyridyl aminoquinoline-benzimidazole hybrid complexes were synthesized and evaluated for their in vitro antiplasmodial activity. The hybrid complexes showed good activity against the chloroquine-sensitive strain of Plasmodium falciparum and maintained activity against the multidrug-resistant strain, with low to no cytotoxicity. Selected active hybrid complexes also demonstrated significant inhibition of beta-haematin formation.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Taryn M. Golding, Reinner O. Omondi, Supratim Biswas, Suparna Chakraborty, Sharon Prince, Gregory S. Smith
Summary: The success of small metal-containing molecules as pharmaceutical agents has led to investigations into the pharmacological activity of supramolecular coordination complexes (SCCs), which have shown promising anticancer activity. The present study evaluated the anticancer activity of quinoline-containing binuclear complexes and metallarectangles in breast cancer cell lines. The results demonstrated that some of these complexes exhibited superior or comparable activity to the clinical chemotherapeutic drugs cisplatin in different breast cancer cell lines. Additionally, the compounds showed increased selectivity towards breast cancer cells over non-tumorigenic cells and displayed favorable binding to DNA and albumin.
Article
Chemistry, Inorganic & Nuclear
Tara K. Davids, Wade F. Petersen, Gregory S. Smith
Summary: A trinuclear bis-cyclometalated iridium(III) polypyridyl complex was synthesized and evaluated as a photoredox catalyst for visible light-mediated thiol-ene coupling reactions. The complex exhibited a blue-shifted emission spectrum and showed promising catalytic activity in photoredox reactions. Compared to a trinuclear ruthenium congener, the trinuclear iridium polypyridyl complex exhibited the highest NMR yields in hydrothiolation coupling reactions.
INORGANIC CHEMISTRY COMMUNICATIONS
(2023)
Article
Biochemistry & Molecular Biology
Stephen de Doncker, Eva Fischer-Fodor, Catalin Ioan Vlad, Patriciu Achimas-Cadariu, Gregory S. Smith, Siyabonga Ngubane
Summary: Two diphenyl formamidine ligands, four dirhodium(II,II) complexes, and three axially modified low-valent dirhodium(II,II) metallodendrimers were synthesized and evaluated for their anticancer activity against ovarian cancer cell lines. The dirhodium(II,II) complexes exhibited moderate cytotoxicity, with acetate and methyl-substituted formamidinate compounds showing increased cytotoxicity compared to cisplatin in the cisplatin resistant cell line. Methyl- and fluoro-substituted formamidinate complexes also demonstrated comparable or increased cytotoxic activity in another cell line. The low-valent metallodendrimers exhibited some activity, but generally showed decreased cytotoxicity compared to the precursor complexes, except for one case where an acetate-derived metallodendrimer showed higher cytotoxicity than dirhodium(II,II) tetraacetate.
Review
Chemistry, Multidisciplinary
Hong Yan, Gregory S. Smith, Fen-Er Chen
Summary: Due to high ring strain energies, cyclopropanols and cyclobutanols have a strong tendency of breaking the endocyclic C-C bonds to participate in versatile organic transformations. Ring-opening asymmetric synthesis of these compounds allows for the synthesis of linear or cyclic molecules with stereogenic centers.
GREEN SYNTHESIS AND CATALYSIS
(2022)
Article
Chemistry, Inorganic & Nuclear
Taryn M. Golding, Mziyanda Mbaba, Gregory S. Smith
Summary: The synthesis of a new ditopic quinoline-based ligand and subsequent metallarectangles showed enhanced antiplasmodial activity in vitro, with an increase in nuclearity correlating with increased activity. The potential of supramolecular metallarectangles as antiplasmodial agents was highlighted, with inhibition of haemozoin formation considered as a potential mechanism of action. Selected metallarectangles exhibited beta-haematin inhibition activity similar to chloroquine.
DALTON TRANSACTIONS
(2021)
Article
Chemistry, Inorganic & Nuclear
Guojun Hu, Ziyue Deng, Yanwei Wang, Dan Yuan, Yong Zhang, Yingming Yao
Summary: A series of rare-earth metal complexes were synthesized and used as efficient initiators for the polymerization of trimethylene carbonate (TMC) and (L)-lactide ((L)-LA).
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2024)
Article
Chemistry, Inorganic & Nuclear
Van Ha Nguyen, John H. K. Yip
Summary: In this study, eight PtII-azulene complexes were synthesized to investigate the effect of metalation on the electronic structures, spectroscopy, and luminescence of organic chromophores. The results showed that the attachment of Pt substituents to azulene affected the HOMOs, LUMOs, and luminescence properties. The study provides insights into the role of metalation in modifying the properties of organic chromophores.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2024)
Article
Chemistry, Inorganic & Nuclear
Moon Kedia, Virender Singh, Bhaskaran Shankar, Malaichamy Sathiyendiran
Summary: This study synthesized two types of neutral binuclear metallocycles using a one-pot solvothermal method and characterized their structures. The analysis revealed that these complexes adopt a binuclear heteroleptic cyclic architecture and belong to phosphine oxide donor (P=O)-based supramolecular coordination cyclic complexes.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2024)
Article
Chemistry, Inorganic & Nuclear
Radhey S. Srivastava
Summary: This study demonstrates the effectiveness of zero-valent elements as reductants for the deoxydehydration reaction of polyols catalyzed by ONO-pincer ligated molybdenum dioxo. The insolubility and easy separability of the reductants and their oxidized products during the reaction are emphasized. Additionally, the choice of ligand has an impact on the catalytic performance of the reaction.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2024)
Article
Chemistry, Inorganic & Nuclear
Hao Zhou, Yajun Sun, Li Deng, Weiran Yang, Yuehui Li
Summary: Efficient Ru-catalyzed hydrogenation of aldehydes was achieved using carbazole-derived phosphine ligands, with the crucial role of N-H moiety in promoting the catalytic reaction. The method was successfully applied in the Co/Ru-catalyzed hydroformylation process, resulting in the production of long-chain alcohols with excellent yields.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2024)
Article
Chemistry, Inorganic & Nuclear
Theodor Danescu, Alexandru Lupan, Radu Silaghi-Dumitrescu, R. Bruce King
Summary: The structures and energies of complexes containing (Me2C2N2P)2Ru2(CO)n and (Me2C2N2P)2Fe2(CO)n have been studied. Low-energy structures are characterized by the presence of bridging diazaphospholyl rings, while higher-energy structures involve different ligand structures.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2024)
Article
Chemistry, Inorganic & Nuclear
Savannah C. Kapper, Aamani Ponnekanti, Jonas Schaab, Tian-yi Li, Christine L. Chung, Gael Ung, Peter I. Djurovich, Mark E. Thompson
Summary: Organometallic iridium complexes with two cyclometalated ligands and one bis-oxazoline derived ancillary ligand were studied. These complexes have emission spanning across the visible and near-ultraviolet region, with moderate to high photoluminescence quantum yields. The (ppy)2Ir(BOX-CN) complexes were resolved into Delta- and Lambda-diastereomers based on solubility differences.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2024)
Article
Chemistry, Inorganic & Nuclear
Zahra Karimi Sangari, Hossein Naeimi
Summary: In this research, a nanostructured CoCuFe2O4 catalyst was prepared using a brief and useful synthetic strategy. This catalyst was used for synthesizing 1,2,4,5-tetrasubstituted imidazole derivatives under ultrasonic irradiation. The approach offers advantages such as high efficiency, short reaction times, simplicity of the reaction medium, accelerated reaction rates, and easier separation and purification of products.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2024)
Article
Chemistry, Inorganic & Nuclear
Rukhsana Gul, Wajid Munir, Ebraheem Abdu Musad Saleh, Shaukat Shujah, Muhammad Sirajuddin, Saira Tabassum, Khalil Ur Rehman, Dilfaraz Khan, Sameerah I. Al-Saeedi, Ehab A. Abdelrahman
Summary: Two new Schiff base ligands were synthesized and used to form copper, nickel, and cobalt complexes. The synthesized compounds were characterized and screened for various biological activities. The metal complexes showed better activities in antibacterial, antifungal, antidiabetic, and antioxidant assays.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2024)
Review
Chemistry, Inorganic & Nuclear
Ahsan Nazir, Pengwei Huo, Ameena Tur Rasool
Summary: This review explores the potential of g-C3N4-based S-scheme heterojunctions in addressing environmental issues. It summarizes the mechanism and preparation techniques of S-scheme heterojunctions based on g-C3N4, and presents recent studies on their applications in pollutant removal, CO2 reduction, hydrogen production, and bacterial disinfection. The review concludes with an outlook on future challenges for g-C3N4-based S-scheme heterojunctions.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2024)
Article
Chemistry, Inorganic & Nuclear
Francois Mazars, Koffi Senam Etse, Guillermo Zaragoza, Lionel Delaude
Summary: The activity of three Pd-PEPPSI catalyst precursors with N-heterocyclic carbene (NHC) ligands derived from caffeine and theophylline in Mizoroki-Heck reactions was tested. The results showed that the catalysts achieved high conversions and yields, especially in the presence of electron-withdrawing substituents.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2024)
Article
Chemistry, Inorganic & Nuclear
Bo-Han Wu, Xue Zhou, Lin Liu, Zheng-Bo Han
Summary: Researching carbon dioxide removal from flue gas and natural gas is crucial. Metal-organic frameworks (MOFs) are commonly used in adsorption due to their high surface area, porosity, and chemical properties. An ultra-microporous MOF CPM-20(Co) with mixed ligand was synthesized using inexpensive ligands. The material exhibited high selectivities and low regenerative energy, making it a promising option for CO2 separation in industries.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2024)