Development of a synthetic strategy for Water soluble tripodal receptors: Two novel fluorescent receptors for highly selective and sensitive detections of Fe3+ and Cu2+ ions and biological evaluation

2020 ◽  
Vol 392 ◽  
pp. 112411 ◽  
Author(s):  
Aylin Uslu ◽  
Elif Özcan ◽  
Süreyya Oğuz Tümay ◽  
Hasan Hüseyin Kazan ◽  
Serkan Yeşilot
Keyword(s):  
Biological Evaluation ◽  
Water Soluble ◽  
Synthetic Strategy

Synthesis and Biological Evaluation of Water-Soluble 2-Boronoethylthio Compounds

1964 ◽  
Vol 7 (5) ◽  
pp. 640-643 ◽  
Author(s):  
D. S. Matteson ◽  
A. H. Soloway ◽  
D. W. Tomlinson ◽  
J. D. Campbell ◽  
G. A. Nixon
Keyword(s):  
Biological Evaluation ◽  
Water Soluble ◽  
Synthesis And Biological Evaluation

scholarly journals Versatile synthesis and biological evaluation of novel 3’-fluorinated purine nucleosides

2015 ◽  
Vol 11 ◽  
pp. 2509-2520 ◽  
Author(s):  
Hang Ren ◽  
Haoyun An ◽  
Paul J Hatala ◽  
William C Stevens ◽  
Jingchao Tao ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Biological Evaluation ◽  
Purine Nucleoside ◽  
Coupling Reactions ◽  
Cell Growth Inhibition ◽  
Cross Coupling Reactions ◽  
Synthetic Strategy ◽  
Cancer Tumor ◽  
Purine Ring ◽  
Synthesis And Biological Evaluation

A unified synthetic strategy accessing novel 3'-fluorinated purine nucleoside derivatives and their biological evaluation were achieved. Novel 3’-fluorinated analogues were constructed from a common 3’-deoxy-3’-fluororibofuranose intermediate. Employing Suzuki and Stille cross-coupling reactions, fifteen 3’-fluororibose purine nucleosides 1–15 and eight 3’-fluororibose 2-chloro/2-aminopurine nucleosides 16–23 with various substituents at position 6 of the purine ring were efficiently synthesized. Furthermore, 3’-fluorine analogs of natural products nebularine and 6-methylpurine riboside were constructed via our convergent synthetic strategy. Synthesized nucleosides were tested against HT116 (colon cancer) and 143B (osteosarcoma cancer) tumor cell lines. We have demonstrated 3’-fluorine purine nucleoside analogues display potent tumor cell growth inhibition activity at sub- or low micromolar concentration.

Cytotoxic and antitumoral activity of N-(9H-purin-6-yl) benzamide derivatives and related water-soluble prodrugs

2021 ◽  
Vol 14 ◽  
Author(s):  
Emeline Cros-Perrial ◽  
Steve Saulnier ◽  
Muhammad Zawwad Raza ◽  
Rémi Charmelot ◽  
David Egron ◽  
...  
Keyword(s):  
Cancer Cell ◽  
Molecular Mechanisms ◽  
Biological Evaluation ◽  
Water Soluble ◽  
Antitumoral Activity ◽  
Cell Cycle Distribution ◽  
Synergistic Activity ◽  
Benzamide Derivatives

Background: The development of small molecules as cancer treatments is still of both interest and importance. Objective: Having synthesized and identified the initial cytotoxic activity of a series of chemically related N-(9H-purin-6-yl) benzamide derivatives, we continued their evaluation on cancer cell models. We also synthesized water-soluble prodrugs of the main compound and performed in vivo experiments. Method: We used organic chemistry to obtain compounds of interest and prodrugs. The biological evaluation included MTT assays, synergy experiments, proliferation assays by CFSE, cell cycle distribution and in vivo antitumoral activity. Results: Our results show activities on cancer cell lines ranging from 3-39 µM for the best compounds, with both induction of apoptosis and decrease in cell proliferation. Two compounds evaluated in vivo showed weak antitumoral activity. In addition, the lead compound and its prodrug had a synergistic activity with the nucleoside analogue fludarabine in vitro and in vivo. Conclusion: Our work allowed us to gain better knowledge on the activity of N-(9H-purin-6-yl) benzamide derivatives and showed new examples of water-soluble prodrugs. More research is warranted to decipher the molecular mechanisms of the molecules.

Water Soluble Coumarin Quaternary Ammonium Chlorides: Synthesis and Biological Evaluation

2020 ◽  
Author(s):  
Mert O. Karataş ◽  
Samir A. A. Noma ◽  
Canbolat Gürses ◽  
Sevgi Balcıoğlu ◽  
Burhan Ateş ◽  
...  
Keyword(s):  
Quaternary Ammonium ◽  
Biological Evaluation ◽  
Water Soluble ◽  
Synthesis And Biological Evaluation

Copper, nickel and zinc complexes of a new water-soluble thiosemicarbazone ligand: Synthesis, characterization, stability and biological evaluation

2017 ◽  
Vol 248 ◽  
pp. 658-667 ◽  
Author(s):  
Seyed Abolfazl Hosseini-Yazdi ◽  
Azadeh Mirzaahmadi ◽  
Ali Akbar Khandar ◽  
Majid Mahdavi ◽  
Arezoo Rahimian ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Zinc Complexes ◽  
Water Soluble ◽  
Copper Nickel ◽  
Thiosemicarbazone Ligand ◽  
Ligand Synthesis

Molecular binding behaviors and thermodynamics of ferrocenyl dimethylaminium derivatives by anionic pillar[5]arene

2015 ◽  
Vol 13 (44) ◽  
pp. 10808-10812 ◽  
Author(s):  
Cui-Fang Zhang ◽  
Sheng-Hua Li ◽  
Cai-Cai Zhang ◽  
Yu Liu
Keyword(s):  
Water Soluble ◽  
Molecular Binding ◽  
Synthetic Strategy

A novel anionic water-soluble pillar[5]arene (4C-WP5A) was synthesized via a convenient synthetic strategy of the direct cyclization of a functionalized hydroquinone monomer.

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