29712-28-5Relevant articles and documents
Biologically active pyridine mono- and bis-phosphonates: Efficient ligands for co-ordination of Cu2+ ions
Boduszek, Bogdan,Dyba, Marcin,Jezowska-Bojczuk, Malgorzata,Kiss, Tamas,Kozlowski, Henryk
, p. 973 - 976 (1997)
Potentiometric and spectroscopic studies on the co-ordination ability of biologically important pyridine mono- and bis-phosphonates have shown that when sterically possible these compounds undergo tridentate co-ordination with Cu2+ ions. The complexes obtained are very stable. When the position of the nitrogen donor is sterically unfavourable the major binding occurs at the bis(phosphonate) site.
Syntheses and evaluation of 68Ga- and 153Sm-labeled DOTA-conjugated bisphosphonate ligand for potential use in detection of skeletal metastases and management of pain arising from skeletal metastases
Chakraborty, Sudipta,Goswami, Dibakar,Chakravarty, Rubel,Mohammed, Sahiralam Khan,Sarma, Haladhar Deb,Dash, Ashutosh
, p. 1618 - 1626 (2018)
This article reports the syntheses and evaluation of 68Ga- and 153Sm-complexes of a new DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid)-conjugated geminal bisphosphonate, DOTA-Bn-SCN-BP, for their potential uses in the early detection of skeletal metastases by imaging and palliation of pain arising from skeletal metastases, respectively. The conjugate was synthesized in high purity following an easily adaptable three-step reaction scheme. Gallium-68- and 153Sm-complexes were prepared in high yield (>98%) and showed excellent in vitro stability in phosphate-buffered saline (PBS) and human serum. Both the complexes showed high affinity for hydroxyapatite particles in in vitro binding study. In biodistribution studies carried out in normal Wistar rats, both the complexes exhibited rapid skeletal accumulation with almost no retention in any other major organ. The newly synthesized molecule DOTA-Bn-SCN-BP would therefore be a promising targeting ligand for the development of radiopharmaceuticals for both imaging skeletal metastases and palliation of pain arising out of it in patients with cancer when radiolabeled with 68Ga and 153Sm, respectively. A systematic comparative evaluation, however, showed that there was no significant improvement of skeletal accumulation of the 153Sm-DOTA-Bn-SCN-BP complex over 153Sm-DOTMP (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetramethylenephosphonic acid) as the later itself demonstrated optimal properties required for an agent for bone pain palliation.
An Improved Synthesis of the Antibiotic Dehydrophos
Jiménez-Andreu, M. Mercedes,Sayago, Francisco J.,Cativiela, Carlos
, p. 3965 - 3973 (2018/07/31)
Within this work an efficient procedure for the synthesis of the vinyl phosphonate tripeptide dehydrophos is described. This procedure constitutes a significant improvement over previously described strategies, since critical transformations in the synthesis of dehydrophos were carried out in only two synthetic steps, with higher yields and under smooth conditions. Thus, the dehydrophosphoalanine residue was generated by means of the Horner–Wadsworth–Emmons reaction of formaldehyde with a peptide bearing an aminomethylbis(phosphonate) moiety, whereas deprotection of the N-terminal position of the thus-obtained dehydrophosphonopeptide and partial hydrolysis of the dimethyl phosphonate residue took place simultaneously. In addition, we confirmed that the chiral integrity of the leucine residue was preserved throughout these transformations.
NOVEL BISPHOSPHONATES AND THEIR USE
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Page/Page column 10, (2015/11/09)
We disclose novel diphosphonic acids or their physiologically admissible salts as well as their use in the production of a drug for inhibiting bone resorption, for the prevention or treatment of osteoporosis.
