Synthesis, characterization and in vitro and in vivo anticancer activity of Pt(iv) derivatives of [Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenanthroline)]
This report describes the synthesis, characterization and biological activity of a series of platinum(iv) derivatives of [Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenanthroline)] (Pt56MeSS) with non-bioactive, lipophilic and bioactive axial ligands. In an attempt to explore the anticancer activity potentia...
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| Veröffentlicht in: | Dalton transactions : an international journal of inorganic chemistry 2017-05, Vol.46 (21), p.7005-7019 |
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| container_issue | 21 |
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| container_title | Dalton transactions : an international journal of inorganic chemistry |
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| creator | Harper, Benjamin W J Petruzzella, Emanuele Sirota, Roman Faccioli, Fernanda Fabiola Aldrich-Wright, Janice R Gandin, Valentina Gibson, Dan |
| description | This report describes the synthesis, characterization and biological activity of a series of platinum(iv) derivatives of [Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenanthroline)] (Pt56MeSS) with non-bioactive, lipophilic and bioactive axial ligands. In an attempt to explore the anticancer activity potential of the Pt(iv) derivatives, 2D and 3D cytotoxic screening and a preliminary in vivo study were performed. The average IC
values of the platinum(iv) derivatives ranged from 1.26 to 5.39 μM, compared with 1.24 μM for Pt56MeSS, suggesting that the axial ligands have a relatively minor effect on the potency of the compounds. Preliminary in vivo studies indicate that the platinum(iv) derivatives of Pt56MeSS are active in vivo and can reduce the tumor to a similar extent to cisplatin. |
| doi_str_mv | 10.1039/c7dt01054k |
| format | Article |
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values of the platinum(iv) derivatives ranged from 1.26 to 5.39 μM, compared with 1.24 μM for Pt56MeSS, suggesting that the axial ligands have a relatively minor effect on the potency of the compounds. Preliminary in vivo studies indicate that the platinum(iv) derivatives of Pt56MeSS are active in vivo and can reduce the tumor to a similar extent to cisplatin.</description><identifier>ISSN: 1477-9226</identifier><identifier>EISSN: 1477-9234</identifier><identifier>DOI: 10.1039/c7dt01054k</identifier><identifier>PMID: 28513693</identifier><language>eng</language><publisher>England</publisher><subject>Anticancer properties ; Biocompatibility ; Derivatives ; In vivo methods and tests ; Ligands ; Screening ; Synthesis ; Tumors</subject><ispartof>Dalton transactions : an international journal of inorganic chemistry, 2017-05, Vol.46 (21), p.7005-7019</ispartof><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c320t-e4463669f95415198d6244a0b1782425b1375497d8447703a364fa74a93345fe3</citedby><cites>FETCH-LOGICAL-c320t-e4463669f95415198d6244a0b1782425b1375497d8447703a364fa74a93345fe3</cites><orcidid>0000-0002-1631-4018</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/28513693$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Harper, Benjamin W J</creatorcontrib><creatorcontrib>Petruzzella, Emanuele</creatorcontrib><creatorcontrib>Sirota, Roman</creatorcontrib><creatorcontrib>Faccioli, Fernanda Fabiola</creatorcontrib><creatorcontrib>Aldrich-Wright, Janice R</creatorcontrib><creatorcontrib>Gandin, Valentina</creatorcontrib><creatorcontrib>Gibson, Dan</creatorcontrib><title>Synthesis, characterization and in vitro and in vivo anticancer activity of Pt(iv) derivatives of [Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenanthroline)]</title><title>Dalton transactions : an international journal of inorganic chemistry</title><addtitle>Dalton Trans</addtitle><description>This report describes the synthesis, characterization and biological activity of a series of platinum(iv) derivatives of [Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenanthroline)] (Pt56MeSS) with non-bioactive, lipophilic and bioactive axial ligands. In an attempt to explore the anticancer activity potential of the Pt(iv) derivatives, 2D and 3D cytotoxic screening and a preliminary in vivo study were performed. The average IC
values of the platinum(iv) derivatives ranged from 1.26 to 5.39 μM, compared with 1.24 μM for Pt56MeSS, suggesting that the axial ligands have a relatively minor effect on the potency of the compounds. Preliminary in vivo studies indicate that the platinum(iv) derivatives of Pt56MeSS are active in vivo and can reduce the tumor to a similar extent to cisplatin.</description><subject>Anticancer properties</subject><subject>Biocompatibility</subject><subject>Derivatives</subject><subject>In vivo methods and tests</subject><subject>Ligands</subject><subject>Screening</subject><subject>Synthesis</subject><subject>Tumors</subject><issn>1477-9226</issn><issn>1477-9234</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><recordid>eNqFkclO6zAUhi0EYt7cB7jKskUN-HiMl1UZBRJIhRVCkZs4ii9pUmw3UnkOHhiX6S5ZnUHf-RbnR-gP4GPAVJ0UsgwYMGfPG2gXmJSpIpRt_vRE7KA97_9hTAjmZBvtkIwDFYruorfpqg218daPkqLWThfBOPuqg-3aRLdlYtukt8F1_4d-3Qdb6LYwLokHNgKrpKuSuzCw_TApo6GPht749fYxrmE6ItP0dDy5HA74SKSlnZtQr5oURoDTRW3aqKxd19jWDJ8O0FalG28Ov-o-ejg_u59cpje3F1eT8U1aUIJDahgTVAhVKc6Ag8pKQRjTeAYyI4zwGVDJmZJlxuIjMNVUsEpLphWljFeG7qPBp3fhupel8SGfW1-YptGt6ZY-BwWcEgGC_45mSklFQJKIHn2iheu8d6bKF87OtVvlgPN1YPlEnt5_BHYd4b9f3uVsbsof9Dsh-g7InY2X</recordid><startdate>20170530</startdate><enddate>20170530</enddate><creator>Harper, Benjamin W J</creator><creator>Petruzzella, Emanuele</creator><creator>Sirota, Roman</creator><creator>Faccioli, Fernanda Fabiola</creator><creator>Aldrich-Wright, Janice R</creator><creator>Gandin, Valentina</creator><creator>Gibson, Dan</creator><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><scope>7SR</scope><scope>7U5</scope><scope>8BQ</scope><scope>8FD</scope><scope>JG9</scope><scope>L7M</scope><orcidid>https://orcid.org/0000-0002-1631-4018</orcidid></search><sort><creationdate>20170530</creationdate><title>Synthesis, characterization and in vitro and in vivo anticancer activity of Pt(iv) derivatives of [Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenanthroline)]</title><author>Harper, Benjamin W J ; Petruzzella, Emanuele ; Sirota, Roman ; Faccioli, Fernanda Fabiola ; Aldrich-Wright, Janice R ; Gandin, Valentina ; Gibson, Dan</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c320t-e4463669f95415198d6244a0b1782425b1375497d8447703a364fa74a93345fe3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2017</creationdate><topic>Anticancer properties</topic><topic>Biocompatibility</topic><topic>Derivatives</topic><topic>In vivo methods and tests</topic><topic>Ligands</topic><topic>Screening</topic><topic>Synthesis</topic><topic>Tumors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Harper, Benjamin W J</creatorcontrib><creatorcontrib>Petruzzella, Emanuele</creatorcontrib><creatorcontrib>Sirota, Roman</creatorcontrib><creatorcontrib>Faccioli, Fernanda Fabiola</creatorcontrib><creatorcontrib>Aldrich-Wright, Janice R</creatorcontrib><creatorcontrib>Gandin, Valentina</creatorcontrib><creatorcontrib>Gibson, Dan</creatorcontrib><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>Engineered Materials Abstracts</collection><collection>Solid State and Superconductivity Abstracts</collection><collection>METADEX</collection><collection>Technology Research Database</collection><collection>Materials Research Database</collection><collection>Advanced Technologies Database with Aerospace</collection><jtitle>Dalton transactions : an international journal of inorganic chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Harper, Benjamin W J</au><au>Petruzzella, Emanuele</au><au>Sirota, Roman</au><au>Faccioli, Fernanda Fabiola</au><au>Aldrich-Wright, Janice R</au><au>Gandin, Valentina</au><au>Gibson, Dan</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis, characterization and in vitro and in vivo anticancer activity of Pt(iv) derivatives of [Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenanthroline)]</atitle><jtitle>Dalton transactions : an international journal of inorganic chemistry</jtitle><addtitle>Dalton Trans</addtitle><date>2017-05-30</date><risdate>2017</risdate><volume>46</volume><issue>21</issue><spage>7005</spage><epage>7019</epage><pages>7005-7019</pages><issn>1477-9226</issn><eissn>1477-9234</eissn><abstract>This report describes the synthesis, characterization and biological activity of a series of platinum(iv) derivatives of [Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenanthroline)] (Pt56MeSS) with non-bioactive, lipophilic and bioactive axial ligands. In an attempt to explore the anticancer activity potential of the Pt(iv) derivatives, 2D and 3D cytotoxic screening and a preliminary in vivo study were performed. The average IC
values of the platinum(iv) derivatives ranged from 1.26 to 5.39 μM, compared with 1.24 μM for Pt56MeSS, suggesting that the axial ligands have a relatively minor effect on the potency of the compounds. Preliminary in vivo studies indicate that the platinum(iv) derivatives of Pt56MeSS are active in vivo and can reduce the tumor to a similar extent to cisplatin.</abstract><cop>England</cop><pmid>28513693</pmid><doi>10.1039/c7dt01054k</doi><tpages>15</tpages><orcidid>https://orcid.org/0000-0002-1631-4018</orcidid></addata></record> |
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| identifier | ISSN: 1477-9226 |
| ispartof | Dalton transactions : an international journal of inorganic chemistry, 2017-05, Vol.46 (21), p.7005-7019 |
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| language | eng |
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| source | Royal Society Of Chemistry Journals; Alma/SFX Local Collection |
| subjects | Anticancer properties Biocompatibility Derivatives In vivo methods and tests Ligands Screening Synthesis Tumors |
| title | Synthesis, characterization and in vitro and in vivo anticancer activity of Pt(iv) derivatives of [Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenanthroline)] |
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