Synthesis and cytotoxicity of N,N′-dibisphosphonate ethylenediamine derivatives and platinum(II) complexes with high binding property to hydroxyapatite

Background: Chromene and anilinopyrimidine heterocyclics are attractive anticancer compounds that have inspired many researchers to design novel derivatives bearing improved anticancer activity. Methods: A series of pyrimidine-fused benzo[f]chromene derivatives 6a-x were synthesized as anticancer hybrids of 1H-benzo[f]chromenes and anilinopyrimidines. The inhibitory activity of the synthesized compounds 6a-x against cell viability of human chronic myelogenous leukemia (K562), human acute lymphoblastic leukemia (MOLT-4) and human breast adenocarcinoma (MCF-7) cell lines was evaluated using MTT assay. The interaction of the most promising compound with calf-thymus DNA was also studied using spectrometric titrations and Circular Dichroism (CD) spectroscopy. Results: Most compounds showed promising activity against tested cell lines. Among them, 2,4- dimethoxyanilino derivative 6g exhibited the best profile of activity against tested cell lines (IC50s = 1.6-6.1 μM) with no toxicity against NIH3T3 normal cell (IC50 >200 μM). The spectrometric studies exhibited that compound 6g binds to DNA strongly and may change DNA conformation significantly, presumably via a groove binding mechanism. Conclusion: The results of this study suggest that the prototype compound 6g can be considered as a novel lead compound for the design and discovery of novel anticancer agents.

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Magnetic Separation of Antibodies with High Binding Capacity by Site-Directed Immobilization of Protein A-Domains to Bare Iron Oxide Nanoparticles

ACS Applied Nano Materials ◽

10.1021/acsanm.1c00487 ◽

2021 ◽

Author(s):

Yasmin Kaveh-Baghbaderani ◽

Raphaela Allgayer ◽

Sebastian Patrick Schwaminger ◽

Paula Fraga-García ◽

Sonja Berensmeier

Keyword(s):

Iron Oxide ◽

Magnetic Separation ◽

Iron Oxide Nanoparticles ◽

Binding Capacity ◽

Protein A ◽

Oxide Nanoparticles ◽

High Binding ◽

A Domains

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The Effect of Hydroxyl on the Superhydrophobicity of Dodecyl Methacrylate (LMA) Coated Fabrics through Simple Dipping-Plasma Crosslinked Method

Coatings ◽

10.3390/coatings10121263 ◽

2020 ◽

Vol 10 (12) ◽

pp. 1263

Author(s):

Liyun Xu ◽

Yu Zhang ◽

Ying Guo ◽

Ruiyun Zhang ◽

Jianjun Shi ◽

...

Keyword(s):

Thermoplastic Polyurethane ◽

Hydrophobic Effect ◽

Surface Hydrophobicity ◽

Contact Angles ◽

Binding Property ◽

Interesting Phenomenon ◽

Water Contact ◽

Capacitively Coupled ◽

Pet Fabric ◽

Dodecyl Methacrylate

In order to obtain stable superhydrophobicity, suitable hydrophobic treatment agents should be selected according to different material properties. In this paper, cotton and poly(ethylene terephthalate) (PET) fabrics were respectively coated with dodecyl methacrylate (LMA) via argon combined capacitively coupled plasma (CCP), and the surface hydrophobicity and durability of the treated cotton and polyester fabrics are also discussed. An interesting phenomenon happened, whereby the LMA-coated cotton fabric (Cotton-g-LMA) had better water repelling and mechanical durability properties than LMA-coated PET fabric (PET-g-LMA), and LMA-coated hydroxyl-grafted PET fabrics (PET fabrics were successively coated with polyethylene glycol (PEG) and LMA, PET-g-PEG & LMA) had a similar performance to cotton fabrics. The water contact angles of Cotton-g-LMA, PET-g-LMA and PET-g-PEG & LMA were 156°, 153° and 155°, respectively, and after 45 washing cycles or 1000 rubbing cycles, the corresponding water contact angles decreased to 145°, 88°, 134° and 146°, 127° and 143°, respectively. Additionally, thermoplastic polyurethane (TPU) and polyamides-6 (PA6) fabrics all exhibited the same properties as the PET fabric. Therefore, the grafting of hydroxyl can improve the hydrophobic effect of LMA coating and the binding property between LMA and fabrics effectively, without changing the wearing comfort.

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Herb-target virtual screening and network pharmacology for prediction of molecular mechanism of Danggui Beimu Kushen Wan for prostate cancer

Scientific Reports ◽

10.1038/s41598-021-86141-1 ◽

2021 ◽

Vol 11 (1) ◽

Author(s):

Hong Li ◽

Andrew Hung ◽

Angela Wei Hong Yang

Keyword(s):

Prostate Cancer ◽

Binding Affinity ◽

Molecular Mechanisms ◽

Biological Activities ◽

Tight Binding ◽

Experimental Studies ◽

Network Pharmacology ◽

High Morbidity ◽

High Binding ◽

High Binding Affinity

AbstractProstate cancer (PCa) is a cancer that occurs in the prostate with high morbidity and mortality. Danggui Beimu Kushen Wan (DBKW) is a classic formula for patients with difficult urination including PCa. This study aimed to investigate the molecular mechanisms of DBKW for PCa. We obtained DBKW compounds from our previous reviews. We identified potential targets for PCa from literature search, currently approved drugs and Open Targets database and filtered them by protein–protein interaction network analysis. We selected 26 targets to predict three cancer-related pathways. A total of 621 compounds were screened via molecular docking using PyRx and AutoDock Vina against 21 targets for PCa, producing 13041 docking results. The binding patterns and positions showed that a relatively small number of tight-binding compounds from DBKW were predicted to interact strongly and selectively with three targets. The top five high-binding-affinity compounds were selected to generate a network, indicating that compounds from all three herbs had high binding affinity against the 21 targets and may have potential biological activities with the targets. DBKW contains multi-targeting agents that could act on more than one pathway of PCa simultaneously. Further studies could focus on validating the computational results via experimental studies.

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Solvent-free and efficient synthesis of bicyclic 2-pyridone derivatives for endoplasmic reticulum imaging

Organic Chemistry Frontiers ◽

10.1039/d1qo00350j ◽

2021 ◽

Author(s):

Xiaoyun Ran ◽

Qian Zhou ◽

Jin Zhang ◽

Shanqiang Wang ◽

Gui Wang ◽

...

Keyword(s):

Endoplasmic Reticulum ◽

Citric Acid ◽

Core Structure ◽

Solvent Free ◽

Efficient Synthesis ◽

The Core ◽

Catalyst Free ◽

Synthesis Approach ◽

Ethylenediamine Derivatives

Started from citric acid (CA) and ethylenediamine derivatives, a solvent-free, catalyst-free and highly yield synthesis approach for bicyclic 2-pyridones was presented. Continuing to modify the core structure, a series of...

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