Stepwise assembly of platinum-folic acid conjugates

Elisabetta Gabano; Mauro Ravera; Claudio Cassino; Samuele Bonetti; Giovanni Palmisano; Domenico Osella

doi:10.1016/j.ica.2007.09.020

Stepwise assembly of platinum-folic acid conjugates

Elisabetta Gabano, Mauro Ravera, Claudio Cassino, Samuele Bonetti, Giovanni Palmisano, Domenico Osella

Research output: Contribution to journal › Article › peer-review

Abstract

Folates and folate-like molecules represent a class of vectors for drug targeting and delivery. The folate receptor (FR) is overexpressed in many human cancers, therefore folate-cytotoxic drug conjugates can deliver therapeutic agents specifically to FR positive tumours. We have linked, directly through one of the carboxylate functionalities of the folic acid (α or γ), two different chelating arms for a cytotoxic platinum moiety, namely a diamine and a dicarboxylate. Five different derivatives were synthesised by multi-step procedures, purified and characterised; unfortunately, they resulted barely soluble in water, thereby precluding any biochemical and biological tests.

Original language	English
Pages (from-to)	1447-1455
Number of pages	9
Journal	Inorganica Chimica Acta
Volume	361
Issue number	5
DOIs	https://doi.org/10.1016/j.ica.2007.09.020
Publication status	Published - 1 Apr 2008

Keywords

Coupling agents
Drug targeting
Folic acid
Kaminski's reaction
Platinum complexes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.ica.2007.09.020

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title = "Stepwise assembly of platinum-folic acid conjugates",

abstract = "Folates and folate-like molecules represent a class of vectors for drug targeting and delivery. The folate receptor (FR) is overexpressed in many human cancers, therefore folate-cytotoxic drug conjugates can deliver therapeutic agents specifically to FR positive tumours. We have linked, directly through one of the carboxylate functionalities of the folic acid (α or γ), two different chelating arms for a cytotoxic platinum moiety, namely a diamine and a dicarboxylate. Five different derivatives were synthesised by multi-step procedures, purified and characterised; unfortunately, they resulted barely soluble in water, thereby precluding any biochemical and biological tests.",

keywords = "Coupling agents, Drug targeting, Folic acid, Kaminski's reaction, Platinum complexes",

author = "Elisabetta Gabano and Mauro Ravera and Claudio Cassino and Samuele Bonetti and Giovanni Palmisano and Domenico Osella",

note = "Funding Information: This work was financially supported by Regione Piemonte. The research was carried out within the framework of the European Cooperation COST D39 (Metallo-Drug Design and Action) and COST B16 action (Multidrug resistance reversal). ",

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AU - Gabano, Elisabetta

AU - Ravera, Mauro

AU - Cassino, Claudio

AU - Bonetti, Samuele

AU - Palmisano, Giovanni

AU - Osella, Domenico

N1 - Funding Information: This work was financially supported by Regione Piemonte. The research was carried out within the framework of the European Cooperation COST D39 (Metallo-Drug Design and Action) and COST B16 action (Multidrug resistance reversal).

PY - 2008/4/1

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N2 - Folates and folate-like molecules represent a class of vectors for drug targeting and delivery. The folate receptor (FR) is overexpressed in many human cancers, therefore folate-cytotoxic drug conjugates can deliver therapeutic agents specifically to FR positive tumours. We have linked, directly through one of the carboxylate functionalities of the folic acid (α or γ), two different chelating arms for a cytotoxic platinum moiety, namely a diamine and a dicarboxylate. Five different derivatives were synthesised by multi-step procedures, purified and characterised; unfortunately, they resulted barely soluble in water, thereby precluding any biochemical and biological tests.

AB - Folates and folate-like molecules represent a class of vectors for drug targeting and delivery. The folate receptor (FR) is overexpressed in many human cancers, therefore folate-cytotoxic drug conjugates can deliver therapeutic agents specifically to FR positive tumours. We have linked, directly through one of the carboxylate functionalities of the folic acid (α or γ), two different chelating arms for a cytotoxic platinum moiety, namely a diamine and a dicarboxylate. Five different derivatives were synthesised by multi-step procedures, purified and characterised; unfortunately, they resulted barely soluble in water, thereby precluding any biochemical and biological tests.

KW - Coupling agents

KW - Drug targeting

KW - Folic acid

KW - Kaminski's reaction

KW - Platinum complexes

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U2 - 10.1016/j.ica.2007.09.020

DO - 10.1016/j.ica.2007.09.020

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JO - Inorganica Chimica Acta

JF - Inorganica Chimica Acta

IS - 5

ER -

Stepwise assembly of platinum-folic acid conjugates

Abstract

Keywords

UN SDGs

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