Structural diversity in aroylthiourea copper complexes – formation and biological evaluation of [Cu(i)(μ-S)SCl]2, cis-Cu(ii)S2O2, trans-Cu(ii)S2O2 and Cu(i)S3 cores

2016 ◽  
Vol 40 (6) ◽  
pp. 5401-5413 ◽  
Author(s):  
Nagamani Selvakumaran ◽  
Lakshmanan Sandhiya ◽  
Nattamai S. P. Bhuvanesh ◽  
Kittusamy Senthilkumar ◽  
Ramasamy Karvembu
Keyword(s):  
Copper Complexes ◽  
Structural Diversity ◽  
Biological Evaluation ◽  
Ct Dna

Four different copper complexes containing aroylthiourea ligands displayed good interaction with CT DNA and BSA and cytotoxicity.

Structural Diversity of Copper Complexes with 2,2′-Dipyridyldisulfide. From Dimer to Infinite Sheet Structure Both in Solid State and in Solution

1998 ◽  
Vol 27 (10) ◽  
pp. 1067-1068 ◽  
Author(s):  
Sachiko Kubo ◽  
Takanori Nishioka ◽  
Keiichirou Ishikawa ◽  
Isamu Kinoshita ◽  
Kiyoshi Isobe
Keyword(s):  
Solid State ◽  
Copper Complexes ◽  
Structural Diversity ◽  
Sheet Structure

scholarly journals Biological and Pharmacological Effects of Synthetic Saponins

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 4974
Author(s):  
Yu-Pu Juang ◽  
Pi-Hui Liang
Keyword(s):  
Biological Activities ◽  
Structural Diversity ◽  
Biological Evaluation ◽  
Steroid Saponin ◽  
Immunomodulatory Effects ◽  
Traditional Medicines ◽  
Amphiphilic Molecules ◽  
Structure Activity ◽  
Recent Developments ◽  
Structure Heterogeneity

Saponins are amphiphilic molecules consisting of carbohydrate and either triterpenoid or steroid aglycone moieties and are noted for their multiple biological activities—Fungicidal, antimicrobial, antiviral, anti-inflammatory, anticancer, antioxidant and immunomodulatory effects have all been observed. Saponins from natural sources have long been used in herbal and traditional medicines; however, the isolation of complexed saponins from nature is difficult and laborious, due to the scarce amount and structure heterogeneity. Chemical synthesis is considered a powerful tool to expand the structural diversity of saponin, leading to the discovery of promising compounds. This review focuses on recent developments in the structure optimization and biological evaluation of synthetic triterpenoid and steroid saponin derivatives. By summarizing the structure–activity relationship (SAR) results, we hope to provide the direction for future development of saponin-based bioactive compounds.

New RuIIpincer complexes: synthesis, characterization and biological evaluation for photodynamic therapy

2016 ◽  
Vol 45 (45) ◽  
pp. 18333-18345 ◽  
Author(s):  
Leila Tabrizi ◽  
Hossein Chiniforoshan
Keyword(s):  
Photodynamic Therapy ◽  
Dna Binding ◽  
Biological Evaluation ◽  
Pincer Complexes ◽  
Dna Photocleavage ◽  
Ct Dna

The CT DNA binding, DNA photocleavage and photocytotoxicity of ruthenium(ii)–NCN pincer complexes were investigated.

Chemical genetics approach to drug discovery by diversity-oriented synthesis (DOS) of peptidomimetics

2011 ◽  
Vol 83 (3) ◽  
pp. 687-698 ◽  
Author(s):  
Andrea Trabocchi ◽  
Duccio Cavalieri ◽  
Antonio Guarna
Keyword(s):  
Drug Discovery ◽  
Small Molecules ◽  
Anticancer Agents ◽  
Structural Diversity ◽  
Chemical Genetics ◽  
Biological Evaluation ◽  
Phenotypic Screening ◽  
Diversity Oriented Synthesis ◽  
Biological Phenotype ◽  
Lead Generation

Chemical genetics, which relies on selecting small molecules for their ability to induce a biological phenotype or to interact with a particular gene product, is a new powerful tool for lead generation in drug discovery. Accordingly, diversity-oriented synthesis (DOS) of small-molecule peptidomimetics gives access to collections of new chemotypes bearing high structural diversity. Biological evaluation using cell growth as a phenotypic screening on Saccharomyces cerevisiae deletant strains is a powerful tool to identify new chemotypes as hit compounds in the discovery of new antifungal and anticancer agents, and also in the dissection of their mode of action. Our contribution in this field focused on the screening of morpholine-based peptidomimetic collections toward yeast deletant strains, which provided the identification of new chemotypes involved in mitochondria metabolism and respiration.

scholarly journals Canvass: A Crowd-Sourced, Natural Product Screening Library for Exploring Biological Space

2018 ◽  
Author(s):  
Sara E. Kearney ◽  
Gergely Zahoránszky-Kőhalmi ◽  
Kyle R. Brimacombe ◽  
Mark J. Henderson ◽  
Caitlin Lynch ◽  
...  
Keyword(s):  
Natural Products ◽  
High Throughput ◽  
High Throughput Screening ◽  
Therapeutic Potential ◽  
Structural Diversity ◽  
Biological Evaluation ◽  
Structural Class ◽  
Differential Behavior ◽  
Biological Potential ◽  
Approved Drugs

Natural products and their derivatives continue to be wellsprings of nascent therapeutic potential. However, many laboratories have limited resources for biological evaluation, leaving their previously isolated or synthesized compounds largely or completely untested. To address this issue, the Canvass library of natural products was assembled, in collaboration with academic and industry researchers, for quantitative high-throughput screening (qHTS) across a diverse set of cell-based and biochemical assays. Characterization of the library in terms of physicochemical properties, structural diversity, and similarity to compounds in publicly available libraries indicates that the Canvass library contains many structural elements in common with approved drugs. The assay data generated were analyzed using a variety of quality control metrics, and the resultant assay profiles were explored using statistical methods, such as clustering and compound promiscuity analyses. Individual compounds were then sorted by structural class and activity profiles. Differential behavior based on these classifications, as well as noteworthy activities, are outlined herein. One such highlight is the activity of (–)-2(<i>S</i>)-cathafoline, which was found to stabilize calcium levels in the endoplasmic reticulum. The workflow described here illustrates a pilot effort to broadly survey the biological potential of natural products by utilizing the power of automation and high-throughput screening.

Structural diversity of copper complexes with angular and linear dipyridyl ligands

Polyhedron ◽  
2007 ◽  
Vol 26 (12) ◽  
pp. 2817-2828 ◽  
Author(s):  
Salomé Delgado ◽  
Agustín Molina-Ontoria ◽  
Manuela E. Medina ◽  
Cesar J. Pastor ◽  
Reyes Jiménez-Aparicio ◽  
...  
Keyword(s):  
Copper Complexes ◽  
Structural Diversity

Discrete and Polymeric Cu(II) Coordination Complexes with a Flexible bis-(pyridylpyrazole) Ligand: Structural Diversity and Unexpected Solvothermal Reactivity

2013 ◽  
Vol 66 (4) ◽  
pp. 401 ◽  
Author(s):  
Chris S. Hawes ◽  
Paul E. Kruger
Keyword(s):  
Coordination Polymer ◽  
Copper Complexes ◽  
Three Dimensional ◽  
Structural Diversity ◽  
Bidentate Ligand ◽  
Two Dimensional ◽  
Ligand Complex ◽  
Structural Characterisation ◽  
Concomitant Reduction ◽  
Pure Phases

Reported here is the synthesis and structural characterisation of five copper complexes derived from the bis-bidentate ligand 4,4′-methylenebis(1-(2-pyridyl)-3,5-dimethylpyrazole), L. Complex 1, [Cu2L(CH3COO)4(OH2)2]·6H2O, is a single stranded unsaturated helical species that forms a highly connected three-dimensional hydrogen-bonding network, whereas [Cu2L(NO3)4], 2, is a coordination polymer derived from [Cu2L] fragments linked together via bridging nitrate anions to yield undulating two-dimensional sheets with (6,3)-topology. Complexes 3, 4, and 5 co-crystallise within a single batch when L is reacted under solvothermal conditions with Cu(NO3)2·2.5H2O in acetonitrile, and each contains a co-ligand formed by either decomposition of the solvent or ligand. Complex 3, [Cu4(NO3)4(µ-CH3COO)2(µ-OH)2L2], forms an unusual discrete cyclic tetrameric species containing acetate co-ligands derived through acetonitrile hydrolysis; whereas complex 4, [CuL(C2O4)(NO3)], forms a one-dimensional coordination polymer containing bridging oxalate co-ligands, formed through hydrolysis and oxidation of acetonitrile. Complex 5, [Cu2L(µ-CN)2], is a two-dimensional coordination polymer with (6,3) topology where bridging between Cu(i) centres is furnished by cyanide co-ligands, suggesting a ligand decomposition pathway for its origin, and produced with concomitant reduction of the Cu(ii) starting reagent. Having initially obtained 3, 4, and 5 serendipitously each were then prepared as pure phases by careful adjustment and control of the reaction conditions (reactant stoichiometry, concentrations, and solvothermal temperature), details of which are discussed.

scholarly journals Canvass: A Crowd-Sourced, Natural Product Screening Library for Exploring Biological Space

2018 ◽  
Author(s):  
Sara E. Kearney ◽  
Gergely Zahoránszky-Kőhalmi ◽  
Kyle R. Brimacombe ◽  
Mark J. Henderson ◽  
Caitlin Lynch ◽  
...  
Keyword(s):  
Natural Products ◽  
High Throughput ◽  
High Throughput Screening ◽  
Therapeutic Potential ◽  
Structural Diversity ◽  
Biological Evaluation ◽  
Structural Class ◽  
Differential Behavior ◽  
Biological Potential ◽  
Approved Drugs

Natural products and their derivatives continue to be wellsprings of nascent therapeutic potential. However, many laboratories have limited resources for biological evaluation, leaving their previously isolated or synthesized compounds largely or completely untested. To address this issue, the Canvass library of natural products was assembled, in collaboration with academic and industry researchers, for quantitative high-throughput screening (qHTS) across a diverse set of cell-based and biochemical assays. Characterization of the library in terms of physicochemical properties, structural diversity, and similarity to compounds in publicly available libraries indicates that the Canvass library contains many structural elements in common with approved drugs. The assay data generated were analyzed using a variety of quality control metrics, and the resultant assay profiles were explored using statistical methods, such as clustering and compound promiscuity analyses. Individual compounds were then sorted by structural class and activity profiles. Differential behavior based on these classifications, as well as noteworthy activities, are outlined herein. One such highlight is the activity of (–)-2(<i>S</i>)-cathafoline, which was found to stabilize calcium levels in the endoplasmic reticulum. The workflow described here illustrates a pilot effort to broadly survey the biological potential of natural products by utilizing the power of automation and high-throughput screening.

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