Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays

A miniaturized assay was optimized to evaluate the enhanced apparent water solubility of pyrazolo[3,4-d]pyrimidine derivatives used extensively as anticancer drug scaffolds. The applied amount of drugs used in the reported strategy ranged from 5-10 μg per formulation which were dispensed by an inkje...

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Main Authors:	Sanna, Monica, Sicilia, Giovanna, Alazzo, Ali, Singh, Nishant, Musumeci, Francesca, Schenone, Silvia, Spriggs, Keith, Burley, Jonathan C., Garnett, Martin, Taresco, Vincenzo, Alexander, Cameron
Format:	Article
Language:	English
Published:	American Chemical Society 2018
Online Access:	http://eprints.nottingham.ac.uk/49478/ http://eprints.nottingham.ac.uk/49478/ http://eprints.nottingham.ac.uk/49478/ http://eprints.nottingham.ac.uk/49478/1/acsmedchemlett.7b00456.pdf

id	nottingham-49478
recordtype	eprints
spelling	nottingham-494782018-07-02T09:18:13Z http://eprints.nottingham.ac.uk/49478/ Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays Sanna, Monica Sicilia, Giovanna Alazzo, Ali Singh, Nishant Musumeci, Francesca Schenone, Silvia Spriggs, Keith Burley, Jonathan C. Garnett, Martin Taresco, Vincenzo Alexander, Cameron A miniaturized assay was optimized to evaluate the enhanced apparent water solubility of pyrazolo[3,4-d]pyrimidine derivatives used extensively as anticancer drug scaffolds. The applied amount of drugs used in the reported strategy ranged from 5-10 μg per formulation which were dispensed by an inkjet 2D printer directly into a 96-well plate. The selected polymer/drug formulations with high water solubility demonstrated improved cytotoxicity against a human lung adenocarcinoma cancer cell line (A549) compared to the free drugs. We attribute the enhanced efficacy to the improved apparent-solubility of the drug molecules achieved via this methodology. This novel miniaturized method showed promising results in terms of water solubility improvement of the highly hydrophobic pyrazolo[3,4-d]pyrimidine derivatives, requiring only a few μg of each drug per tested polymeric formulation. In addition, the reported experimental evidence may facilitate identification of suitable polymers for combination with drug leading to investigations on biological properties or mechanisms of action in a single formulation. American Chemical Society 2018-01-29 Article PeerReviewed application/pdf en http://eprints.nottingham.ac.uk/49478/1/acsmedchemlett.7b00456.pdf Sanna, Monica and Sicilia, Giovanna and Alazzo, Ali and Singh, Nishant and Musumeci, Francesca and Schenone, Silvia and Spriggs, Keith and Burley, Jonathan C. and Garnett, Martin and Taresco, Vincenzo and Alexander, Cameron (2018) Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays. ACS Medicinal Chemistry Letters, 9 (3). pp. 193-197. ISSN 1948-5875 http://pubs.acs.org/doi/10.1021/acsmedchemlett.7b00456 doi:10.1021/acsmedchemlett.7b00456 doi:10.1021/acsmedchemlett.7b00456
repository_type	Digital Repository
institution_category	Local University
institution	University of Nottingham Malaysia Campus
building	Nottingham Research Data Repository
collection	Online Access
language	English
description	A miniaturized assay was optimized to evaluate the enhanced apparent water solubility of pyrazolo[3,4-d]pyrimidine derivatives used extensively as anticancer drug scaffolds. The applied amount of drugs used in the reported strategy ranged from 5-10 μg per formulation which were dispensed by an inkjet 2D printer directly into a 96-well plate. The selected polymer/drug formulations with high water solubility demonstrated improved cytotoxicity against a human lung adenocarcinoma cancer cell line (A549) compared to the free drugs. We attribute the enhanced efficacy to the improved apparent-solubility of the drug molecules achieved via this methodology. This novel miniaturized method showed promising results in terms of water solubility improvement of the highly hydrophobic pyrazolo[3,4-d]pyrimidine derivatives, requiring only a few μg of each drug per tested polymeric formulation. In addition, the reported experimental evidence may facilitate identification of suitable polymers for combination with drug leading to investigations on biological properties or mechanisms of action in a single formulation.
format	Article
author	Sanna, Monica Sicilia, Giovanna Alazzo, Ali Singh, Nishant Musumeci, Francesca Schenone, Silvia Spriggs, Keith Burley, Jonathan C. Garnett, Martin Taresco, Vincenzo Alexander, Cameron
spellingShingle	Sanna, Monica Sicilia, Giovanna Alazzo, Ali Singh, Nishant Musumeci, Francesca Schenone, Silvia Spriggs, Keith Burley, Jonathan C. Garnett, Martin Taresco, Vincenzo Alexander, Cameron Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays
author_facet	Sanna, Monica Sicilia, Giovanna Alazzo, Ali Singh, Nishant Musumeci, Francesca Schenone, Silvia Spriggs, Keith Burley, Jonathan C. Garnett, Martin Taresco, Vincenzo Alexander, Cameron
author_sort	Sanna, Monica
title	Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays
title_short	Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays
title_full	Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays
title_fullStr	Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays
title_full_unstemmed	Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays
title_sort	water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays
publisher	American Chemical Society
publishDate	2018
url	http://eprints.nottingham.ac.uk/49478/ http://eprints.nottingham.ac.uk/49478/ http://eprints.nottingham.ac.uk/49478/ http://eprints.nottingham.ac.uk/49478/1/acsmedchemlett.7b00456.pdf
first_indexed	2018-09-06T14:06:50Z
last_indexed	2018-09-06T14:06:50Z
_version_	1610867341063618560

Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays

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