Article
Chemistry, Inorganic & Nuclear
Eunice A. Nyawade, Nicole R. S. Sibuyi, Mervin Meyer, Roger Lalancette, Martin O. Onani
Summary: New thiosemicarbazone ligands were synthesized and coordinated with palladium to form complexes. The ligands and complexes were characterized using various methods, revealing different coordination modes for different ligands. Conductivity measurements in dimethyl sulfoxide indicated that chloride ions were coordinated within the complexes.
INORGANICA CHIMICA ACTA
(2021)
Article
Biochemistry & Molecular Biology
Jeyce Kelle Ferreira de Andrade, Alexandre Jose da Silva Goes, Vanessa Xavier Barbosa, Mariza Severina de Lima Silva, Mariana Aragao Matos Donato, Christina Alves Peixoto, Gardenia Carmen Gadelha Militao, Teresinha Goncalves da Silva
Summary: Thiosemicarbazones derived from beta-lapachone showed potent cytotoxic effects on leukemia cells, with BV3 being the most selective compound, exhibiting high toxicity to tumor cells and low toxicity to normal cells. These compounds have the potential to be promising candidates for anticancer drugs.
CHEMICO-BIOLOGICAL INTERACTIONS
(2022)
Article
Chemistry, Inorganic & Nuclear
Wycliffe Odhiambo Misigo, Lydia Wanjiru Njenga, Ruth Akech Odhiambo, Mervin Meyer, Lauren Julius, Nicole Sibuyi, Roger A. Lalancette, Martin Opiyo Onani
Summary: Novel thiophene-based thiosemicarbazone ligands were synthesized and their corresponding complexes were formed by coordination to Pd ions. These complexes showed good anticancer activities against human cancer cell lines, with L1 exhibiting the best performance. The complexes exhibited higher toxicity towards the cell lines compared to the ligands, with C2 complex showing the highest anticancer activity among all the complexes.
INORGANICA CHIMICA ACTA
(2023)
Review
Chemistry, Medicinal
Cesar Emiliano Hoffmann da Silva, Grace Gosmann, Saulo Fernandes de Andrade
Summary: This review summarizes the synthetic methods and strategies for obtaining anticancer derivatives of limonene and perillyl alcohol from 2000 to 2020, discusses the structure-activity relationships of the most active derivatives, and illustrates potential anticancer compounds.
MINI-REVIEWS IN MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Vida Mashayekhi, Kamaleddin Haj Mohammad Ebrahim Tehrani, Parisa Azerang, Soroush Sardari, Farzad Kobarfard
Summary: In this study, a series of novel 1-substituted indole-3-carboxaldehyde thiosemicarbazones were synthesized as potential antimycobacterial and anticancer agents. Two derivatives showed significant antimycobacterial activity, while four others showed considerable inhibitory effects on cancer cell lines.
ARCHIVES OF PHARMACAL RESEARCH
(2021)
Article
Chemistry, Inorganic & Nuclear
Chinmoy Biswas, Arnab Chatterjee, Vinu Vijayan, Chandra Shekhar Purohit, Manikantan Syamala Kiran, Rajarshi Ghosh
Summary: This article reports the synthesis and structural characterization of a dinuclear silver(I) complex 1, which exhibits selective anticancer activity against liver cancer cells. The anticancer activity of 1 is achieved through induction of mitochondrial death via Reactive Oxygen Species (ROS).
INORGANIC CHEMISTRY COMMUNICATIONS
(2022)
Article
Chemistry, Physical
Savina Savir, Jonathan Wee Kent Liew, Indra Vythilingam, Yvonne Ai Lian Lim, Chun Hoe Tan, Kae Shin Sim, Vannajan Sanghiran Lee, Mohd Jamil Maah, Kong Wai Tan
Summary: The synthesized Schiff base metal complexes exhibited cytotoxicity against human colorectal carcinoma HCT 116 and antiplasmodial activity. The biological activities were influenced by factors such as the hydrophobicity of the substituent groups and the interaction with DNA base pairs.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Chemistry, Medicinal
Joao Franco Machado, Fernanda Marques, Teresa Pinheiro, Maria J. Villa J. de Brito, Gonzalo Scalese, Leticia Perez-Diaz, Lucia Otero, Joao P. M. Antonio, Dinorah Gambino, Tania S. Morais
Summary: Four new Cu(I) complexes were synthesized and characterized, and their anti-trypanosome and anticancer activities were evaluated. The complexes showed higher cytotoxicity against T. cruzi and chemoresistant prostate PC3 cells compared to benchmark drugs nifurtimox and cisplatin. They also exhibited high cellular internalization and activation of apoptosis in ovarian OVCAR3 cells. However, the production of reactive oxygen species was not significant.
Article
Chemistry, Applied
Carolane M. Almeida, Pedro H. S. Marcon, Erica C. M. Nascimento, Joao B. L. Martins, Marcio A. S. Chagas, Mahmi Fujimori, Patricia G. F. De Marchi, Eduardo L. Franca, Adenilda C. Honorio-Franca, Claudia C. Gatto
Summary: This study documented the synthesis and characterization of two new organometallic Au (III) and Pt (II) complexes with 2-acetylthiophene-N(3)-methylthiosemicarbazone (HL). The compounds were characterized using various spectroscopic techniques including X-ray diffraction and MS. The results revealed the coordination of the thiosemicarbazone ligand to the Au (III) and Pt (II) metal atoms in a tridentate mode. The compounds exhibited interactions in their molecular packing, as demonstrated by quantitative analysis of the 3D Hirshfeld surface and 2D fingerprint results. The biological activity of the compounds against MCF-7 human cancer cells was evaluated, and their inhibitory activity was predicted using molecular docking.
APPLIED ORGANOMETALLIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Md Nur Alam, Mohammad Ali Moni, Jun Q. Yu, Philip Beale, Peter Turner, Nick Proschogo, Mohammad Azizur Rahman, M. Pear Hossain, Fazlul Huq
Summary: The palladium complex NH3 showed higher anticancer activity compared to cisplatin, especially in cisplatin-resistant cell lines and colorectal cancer cell lines.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Inorganic & Nuclear
Elisa Palma, Paula Raposinho, Maria Paula Cabral Campello, Dulce Belo, Joana F. Guerreiro, Vitor Alves, Alexandra Fonseca, Antero J. Abrunhosa, Antonio Paulo, Filipa Mendes
Summary: The study explores a new family of BTSC ligands and their copper complexes with improved water-solubility, lower lipophilicity, more negative redox potential, and enhanced cellular uptake efficiency. The cytotoxic evaluation in cancer cells lines and detailed uptake studies suggest the potential of CuGTSMpip as a promising anticancer metallodrug.
EUROPEAN JOURNAL OF INORGANIC CHEMISTRY
(2021)
Review
Chemistry, Medicinal
Zi-wei Zeng, Di Chen, Lei Chen, Bin He, Yan Li
Summary: Artemisinin, an important ingredient of artemisia annua, has been traditionally used for malaria therapy in China for hundreds of years. Recent research has also revealed the anticancer properties of artemisinin and its derivatives. This review summarizes the development of artemisinin and its derivatives as anticancer agents, including natural and synthetic monomers as well as their dimers. It also discusses the mechanisms of action and clinical trials of artemisinin-based drugs for cancer treatment, providing valuable insights for the development of novel anticancer drugs.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Mohit K. Tiwari, Paolo Coghi, Prakhar Agrawal, Dharmendra K. Yadav, Li Jun Yang, Qiu Congling, Dinkar Sahal, Vincent Kam Wai Wong, Sandeep Chaudhary
Summary: A series of lipophilic, halogenated-arylvinyl-1,2,4-trioxanes were synthesized and evaluated for their in vitro anti-plasmodial activity, with ten analogues showing potent activity and selective potential against Plasmodium cells. The most active compound, arylvinyl-1,2,4-trioxane 8f(2), exhibited significant cytotoxic potential in comparison to standard drugs against lung cancer cell lines. Furthermore, in-silico docking studies demonstrated strong virtual interaction of the potent halogenated 1,2,4-trioxanes with the epidermal growth factor receptor.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Inorganic & Nuclear
Jai Devi, Binesh Kumar, Bharti Taxak
Summary: Cancer is a leading cause of death worldwide. Organotin(IV) complexes have shown potential in cancer treatment, while ligands such as thiosemicarbazones and hydrazones can form stable complexes with tin metal, exhibiting significant biological activities.
INORGANIC CHEMISTRY COMMUNICATIONS
(2022)
Article
Chemistry, Physical
Ahmed A. E. Mourad, Youstina W. Rizzk, Islam Zaki, Faten Z. Mohammed, Mohammed El Behery
Summary: A series of hybrid organic nitrogen compounds were synthesized and confirmed through spectroscopic techniques, showing potent antitumor activity by inducing cell cycle arrest and apoptosis in cancer cells. The compounds also exhibited strong inhibitory effects against beta-tubulin polymerization and topoisomerase up enzyme.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
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
Chayan Pandya, Rakesh R. Panicker, Parth Senjaliya, M. K. Hima Hareendran, P. V. Anju, Sibasis Sarkar, Haamid Bhat, Prakash C. Jha, Koya Prabhakara Rao, Gregory S. Smith, Akella Sivaramakrishna
Summary: The study found that the nature of phosphine ligands plays a significant role in the isomerization of 1-alkenes, with chelated diphosphine leading to a relatively faster completion of internal isomerization reaction. Density functional theory calculations indicate that the reaction rate is linked to the relative stability of 1, 2, and 3, with the least stable 3 showing the highest reaction rate.
INORGANICA CHIMICA ACTA
(2021)
Article
Chemistry, Physical
Athi Welsh, Mziyanda Mbaba, Sharon Prince, Gregory S. Smith
Summary: This study describes the synthesis of 2-ferrocenylbenzimidazole metallofragments with varying substituents in the 5-position of a benzimidazole scaffold, and investigates their potential interactions with proteins. The trinuclear complexes showed higher affinity and superior binding energies compared to monomeric congeners, and some synthesized compounds exhibited moderate cytotoxic activity against breast cancer cell lines.
JOURNAL OF MOLECULAR STRUCTURE
(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)