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Ring‐and side‐chain‐substituted MIBG analogues
Author(s) -
Vaidyanathan G.,
Shankar S.,
Affleck D. J.,
Slade S. A.,
Welsh P.,
Zalutsky M. R.
Publication year - 2001
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.25804401114
Subject(s) - chemistry , lipophilicity , neuroblastoma , adrenal medulla , side chain , substituent , in vitro , ring (chemistry) , stereochemistry , pheochromocytoma , biochemistry , endocrinology , cell culture , catecholamine , organic chemistry , medicine , genetics , biology , polymer
In our effort to develop an MIBG analogue with optimised targeting capabilites, we have synthesized a number of ring‐ and side‐chain substituted analogues of MIBG and evaluated their lipophilicity, stability in vitro, uptake in SK‐N‐SH human neuroblastoma cells and tissue distribution in normal mice. Previously, uptake similar to or higher than that for MIBG in canine adrenal medulla and pheochromocytoma patients has been reported for 4‐amino‐3‐iodobenzylguanidine ( p AIBG) and 4‐hydroxy‐3‐iodobenzylguanidine (HIBG), which are polar substituent‐containing MIBG derivatives (1, 2). However, these two compounds have not been evaluated with respect to their uptake in neuroblastoma cells in vitro. The novel compounds developed in this study were evaluated in comparison with HIBG and p AIBG.