A new biotin derivative-DOTA conjugate as a candidate for pretargeted diagnosis and therapy of tumors

Giuseppina Sabatino, Marco Chinol, Giovanni Paganelli, Stefano Papi, Mario Chelli, Giuseppe Leone, Anna Maria Papini, Angelo De Luca, Mauro Ginanneschi

Research output: Contribution to journalArticle

41 Citations (Scopus)

Abstract

The synthesis of a new biotin derivative, the (CO) reduced N-aminohexyl biotinamido derivative, designed to be serum biotinidase resistant, and its conjugation to the chelator DOTA through an amide bond at one of the four carboxymethyl chains are described. The 90Y-labeled conjugate was able to bind avidin at different Av/conjugate molar ratios with good results. The preclinical results indicate that this new biotin-DOTA conjugate is a good candidate for pretargeted diagnosis and therapy of tumors.

Original languageEnglish
Pages (from-to)3170-3173
Number of pages4
JournalJournal of Medicinal Chemistry
Volume46
Issue number14
DOIs
Publication statusPublished - Jul 3 2003

Fingerprint

Biotinidase
Avidin
Carbon Monoxide
Chelating Agents
Biotin
Amides
Tumors
Derivatives
Serum
Neoplasms
Therapeutics
DOTA-biotin

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

A new biotin derivative-DOTA conjugate as a candidate for pretargeted diagnosis and therapy of tumors. / Sabatino, Giuseppina; Chinol, Marco; Paganelli, Giovanni; Papi, Stefano; Chelli, Mario; Leone, Giuseppe; Papini, Anna Maria; De Luca, Angelo; Ginanneschi, Mauro.

In: Journal of Medicinal Chemistry, Vol. 46, No. 14, 03.07.2003, p. 3170-3173.

Research output: Contribution to journalArticle

Sabatino, G, Chinol, M, Paganelli, G, Papi, S, Chelli, M, Leone, G, Papini, AM, De Luca, A & Ginanneschi, M 2003, 'A new biotin derivative-DOTA conjugate as a candidate for pretargeted diagnosis and therapy of tumors', Journal of Medicinal Chemistry, vol. 46, no. 14, pp. 3170-3173. https://doi.org/10.1021/jm030789z
Sabatino, Giuseppina ; Chinol, Marco ; Paganelli, Giovanni ; Papi, Stefano ; Chelli, Mario ; Leone, Giuseppe ; Papini, Anna Maria ; De Luca, Angelo ; Ginanneschi, Mauro. / A new biotin derivative-DOTA conjugate as a candidate for pretargeted diagnosis and therapy of tumors. In: Journal of Medicinal Chemistry. 2003 ; Vol. 46, No. 14. pp. 3170-3173.
@article{5b86e1cec55e42f095626fffd14b7ca6,
title = "A new biotin derivative-DOTA conjugate as a candidate for pretargeted diagnosis and therapy of tumors",
abstract = "The synthesis of a new biotin derivative, the (CO) reduced N-aminohexyl biotinamido derivative, designed to be serum biotinidase resistant, and its conjugation to the chelator DOTA through an amide bond at one of the four carboxymethyl chains are described. The 90Y-labeled conjugate was able to bind avidin at different Av/conjugate molar ratios with good results. The preclinical results indicate that this new biotin-DOTA conjugate is a good candidate for pretargeted diagnosis and therapy of tumors.",
author = "Giuseppina Sabatino and Marco Chinol and Giovanni Paganelli and Stefano Papi and Mario Chelli and Giuseppe Leone and Papini, {Anna Maria} and {De Luca}, Angelo and Mauro Ginanneschi",
year = "2003",
month = "7",
day = "3",
doi = "10.1021/jm030789z",
language = "English",
volume = "46",
pages = "3170--3173",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "14",

}

TY - JOUR

T1 - A new biotin derivative-DOTA conjugate as a candidate for pretargeted diagnosis and therapy of tumors

AU - Sabatino, Giuseppina

AU - Chinol, Marco

AU - Paganelli, Giovanni

AU - Papi, Stefano

AU - Chelli, Mario

AU - Leone, Giuseppe

AU - Papini, Anna Maria

AU - De Luca, Angelo

AU - Ginanneschi, Mauro

PY - 2003/7/3

Y1 - 2003/7/3

N2 - The synthesis of a new biotin derivative, the (CO) reduced N-aminohexyl biotinamido derivative, designed to be serum biotinidase resistant, and its conjugation to the chelator DOTA through an amide bond at one of the four carboxymethyl chains are described. The 90Y-labeled conjugate was able to bind avidin at different Av/conjugate molar ratios with good results. The preclinical results indicate that this new biotin-DOTA conjugate is a good candidate for pretargeted diagnosis and therapy of tumors.

AB - The synthesis of a new biotin derivative, the (CO) reduced N-aminohexyl biotinamido derivative, designed to be serum biotinidase resistant, and its conjugation to the chelator DOTA through an amide bond at one of the four carboxymethyl chains are described. The 90Y-labeled conjugate was able to bind avidin at different Av/conjugate molar ratios with good results. The preclinical results indicate that this new biotin-DOTA conjugate is a good candidate for pretargeted diagnosis and therapy of tumors.

UR - http://www.scopus.com/inward/record.url?scp=0038482100&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0038482100&partnerID=8YFLogxK

U2 - 10.1021/jm030789z

DO - 10.1021/jm030789z

M3 - Article

C2 - 12825956

AN - SCOPUS:0038482100

VL - 46

SP - 3170

EP - 3173

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 14

ER -