Biological Evaluation of Thrombus Imaging Agents Utilizing Water Soluble Phosphines and Tricine as Coligands When Used To Label a Hydrazinonicotinamide-Modified Cyclic Glycoprotein IIb/IIIa Receptor Antagonist with99mTc

1997 ◽  
Vol 8 (2) ◽  
pp. 155-160 ◽  
Author(s):  
John A. Barrett ◽  
Andrew C. Crocker ◽  
David J. Damphousse ◽  
Stuart J. Heminway ◽  
Shuang Liu ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Biological Evaluation ◽  
Water Soluble ◽  
Imaging Agents ◽  
Thrombus Imaging ◽  
Water Soluble Phosphines

scholarly journals Radiosynthesis and biological evaluation of [18F]R91150, a selective 5-HT2A receptor antagonist for PET imaging

2021 ◽  
Vol 96-97 ◽  
pp. S35-S36
Author(s):  
Michael Willmann ◽  
Julian Hegger ◽  
Bernd Neumaier ◽  
Johannes Ermert
Keyword(s):  
Receptor Antagonist ◽  
Pet Imaging ◽  
Biological Evaluation

ChemInform Abstract: Approaches to New Water-Soluble Phosphines.

ChemInform ◽  
2010 ◽  
Vol 23 (49) ◽  
pp. no-no
Author(s):  
T. N. MITCHELL ◽  
K. HEESCHE-WAGNER
Keyword(s):  
Water Soluble ◽  
Water Soluble Phosphines

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

ChemInform Abstract: Construction of Water-Soluble Phosphines: New Advances in Aqueous Organometallic Chemistry

ChemInform ◽  
2010 ◽  
Vol 31 (9) ◽  
pp. no-no
Author(s):  
Kattesh V. Katti ◽  
Douglas E. Berning ◽  
Charles J. Smith ◽  
Hariprasad Gali
Keyword(s):  
Organometallic Chemistry ◽  
Water Soluble ◽  
Water Soluble Phosphines

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.

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