BLEDTA II: Synthesis of a new tumor-visualizing derivative of Co(III)-bleomycin

L. H. DeRiemer, C. F. Meares, D. A. Goodwin, C. I. Diamanti

Research output: Contribution to journal › Article

68 Citations (Scopus)

Abstract

A new bifunctional chelating agent, (S)-1-(p-bromoacetamidobenzyl) ethylenedinitrilotetraacetic acid, has been prepared from L-phenylalanine. Reaction of the chelating agent with the Co(III) complex of the antitumor antibody bleomycin-A2DM was used to generate a new derivative of Co(III)-bleomyin, BLEDTA II. The product can be radiolabeled quickly by binding a radioactive metal ion to the EDTA group. The in vivo distribution of 111In-BLEDTA II in tumor-bearing mice was determined and found to be indistinguishable from that of the clinically useful 111In(III)-BLEDTA I complex.

Original languageEnglish (US)
Pages (from-to)1517-1534
Number of pages18
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume18
Issue number10
StatePublished - 1981

Fingerprint

Bleomycin
Tumors
Chelating Agents
Derivatives
Edetic Acid
Bearings (structural)
Neoplasms
Phenylalanine
Metal ions
Metals
Ions
Antibodies
BLEDTA

ASJC Scopus subject areas

  • Clinical Biochemistry
  • Molecular Medicine
  • Analytical Chemistry
  • Organic Chemistry
  • Drug Discovery
  • Pharmacology

Cite this

DeRiemer, L. H., Meares, C. F., Goodwin, D. A., & Diamanti, C. I. (1981). BLEDTA II: Synthesis of a new tumor-visualizing derivative of Co(III)-bleomycin. Journal of Labelled Compounds and Radiopharmaceuticals, 18(10), 1517-1534.

BLEDTA II : Synthesis of a new tumor-visualizing derivative of Co(III)-bleomycin. / DeRiemer, L. H.; Meares, C. F.; Goodwin, D. A.; Diamanti, C. I.

In: Journal of Labelled Compounds and Radiopharmaceuticals, Vol. 18, No. 10, 1981, p. 1517-1534.

Research output: Contribution to journal › Article

DeRiemer, LH, Meares, CF, Goodwin, DA & Diamanti, CI 1981, 'BLEDTA II: Synthesis of a new tumor-visualizing derivative of Co(III)-bleomycin', Journal of Labelled Compounds and Radiopharmaceuticals, vol. 18, no. 10, pp. 1517-1534.
DeRiemer LH, Meares CF, Goodwin DA, Diamanti CI. BLEDTA II: Synthesis of a new tumor-visualizing derivative of Co(III)-bleomycin. Journal of Labelled Compounds and Radiopharmaceuticals. 1981;18(10):1517-1534.
DeRiemer, L. H. ; Meares, C. F. ; Goodwin, D. A. ; Diamanti, C. I. / BLEDTA II : Synthesis of a new tumor-visualizing derivative of Co(III)-bleomycin. In: Journal of Labelled Compounds and Radiopharmaceuticals. 1981 ; Vol. 18, No. 10. pp. 1517-1534.
@article{7aadb3c44471441f9c9510a91c05ca33,
title = "BLEDTA II: Synthesis of a new tumor-visualizing derivative of Co(III)-bleomycin",
abstract = "A new bifunctional chelating agent, (S)-1-(p-bromoacetamidobenzyl) ethylenedinitrilotetraacetic acid, has been prepared from L-phenylalanine. Reaction of the chelating agent with the Co(III) complex of the antitumor antibody bleomycin-A2DM was used to generate a new derivative of Co(III)-bleomyin, BLEDTA II. The product can be radiolabeled quickly by binding a radioactive metal ion to the EDTA group. The in vivo distribution of 111In-BLEDTA II in tumor-bearing mice was determined and found to be indistinguishable from that of the clinically useful 111In(III)-BLEDTA I complex.",
author = "DeRiemer, {L. H.} and Meares, {C. F.} and Goodwin, {D. A.} and Diamanti, {C. I.}",
year = "1981",
language = "English (US)",
volume = "18",
pages = "1517--1534",
journal = "Journal of Labelled Compounds and Radiopharmaceuticals",
issn = "0362-4803",
publisher = "John Wiley and Sons Ltd",
number = "10",

}

TY - JOUR

T1 - BLEDTA II

T2 - Synthesis of a new tumor-visualizing derivative of Co(III)-bleomycin

AU - DeRiemer, L. H.

AU - Meares, C. F.

AU - Goodwin, D. A.

AU - Diamanti, C. I.

PY - 1981

Y1 - 1981

N2 - A new bifunctional chelating agent, (S)-1-(p-bromoacetamidobenzyl) ethylenedinitrilotetraacetic acid, has been prepared from L-phenylalanine. Reaction of the chelating agent with the Co(III) complex of the antitumor antibody bleomycin-A2DM was used to generate a new derivative of Co(III)-bleomyin, BLEDTA II. The product can be radiolabeled quickly by binding a radioactive metal ion to the EDTA group. The in vivo distribution of 111In-BLEDTA II in tumor-bearing mice was determined and found to be indistinguishable from that of the clinically useful 111In(III)-BLEDTA I complex.

AB - A new bifunctional chelating agent, (S)-1-(p-bromoacetamidobenzyl) ethylenedinitrilotetraacetic acid, has been prepared from L-phenylalanine. Reaction of the chelating agent with the Co(III) complex of the antitumor antibody bleomycin-A2DM was used to generate a new derivative of Co(III)-bleomyin, BLEDTA II. The product can be radiolabeled quickly by binding a radioactive metal ion to the EDTA group. The in vivo distribution of 111In-BLEDTA II in tumor-bearing mice was determined and found to be indistinguishable from that of the clinically useful 111In(III)-BLEDTA I complex.

UR - http://www.scopus.com/inward/record.url?scp=0019774384&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0019774384&partnerID=8YFLogxK

M3 - Article

AN - SCOPUS:0019774384

VL - 18

SP - 1517

EP - 1534

JO - Journal of Labelled Compounds and Radiopharmaceuticals

JF - Journal of Labelled Compounds and Radiopharmaceuticals

SN - 0362-4803

IS - 10

ER -

Access to Document