{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,3,3]],"date-time":"2026-03-03T02:01:48Z","timestamp":1772503308761,"version":"3.50.1"},"reference-count":28,"publisher":"Wiley","issue":"3","license":[{"start":{"date-parts":[[2018,5,30]],"date-time":"2018-05-30T00:00:00Z","timestamp":1527638400000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Chem Biol Drug Des"],"published-print":{"date-parts":[[2018,9]]},"abstract":"<jats:p>This article reports the syntheses and evaluation of <jats:sup>68<\/jats:sup>Ga\u2010 and <jats:sup>153<\/jats:sup>Sm\u2010complexes of a new <jats:styled-content style=\"fixed-case\">DOTA<\/jats:styled-content> (1,4,7,10\u2010tetraazacyclododecane\u20101,4,7,10\u2010tetraacetic acid)\u2010conjugated geminal bisphosphonate, <jats:styled-content style=\"fixed-case\">DOTA<\/jats:styled-content>\u2010Bn\u2010<jats:styled-content style=\"fixed-case\">SCN<\/jats:styled-content>\u2010<jats:styled-content style=\"fixed-case\">BP<\/jats:styled-content>, 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\u2010step reaction scheme. Gallium\u201068\u2010 and <jats:sup>153<\/jats:sup>Sm\u2010complexes were prepared in high yield (&gt;98%) and showed excellent in vitro stability in phosphate\u2010buffered saline (<jats:styled-content style=\"fixed-case\">PBS<\/jats:styled-content>) 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 <jats:styled-content style=\"fixed-case\">DOTA<\/jats:styled-content>\u2010Bn\u2010<jats:styled-content style=\"fixed-case\">SCN<\/jats:styled-content>\u2010<jats:styled-content style=\"fixed-case\">BP<\/jats:styled-content> 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 <jats:sup>68<\/jats:sup>Ga and <jats:sup>153<\/jats:sup>Sm, respectively. A systematic comparative evaluation, however, showed that there was no significant improvement of skeletal accumulation of the <jats:sup>153<\/jats:sup>Sm\u2010<jats:styled-content style=\"fixed-case\">DOTA<\/jats:styled-content>\u2010Bn\u2010<jats:styled-content style=\"fixed-case\">SCN<\/jats:styled-content>\u2010<jats:styled-content style=\"fixed-case\">BP<\/jats:styled-content> complex over <jats:sup>153<\/jats:sup>Sm\u2010<jats:styled-content style=\"fixed-case\">DOTMP<\/jats:styled-content> (1,4,7,10\u2010tetraazacyclododecane\u20101,4,7,10\u2010tetramethylenephosphonic acid) as the later itself demonstrated optimal properties required for an agent for bone pain palliation.<\/jats:p>","DOI":"10.1111\/cbdd.13327","type":"journal-article","created":{"date-parts":[[2018,5,5]],"date-time":"2018-05-05T08:59:59Z","timestamp":1525510799000},"page":"1618-1626","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":11,"title":["Syntheses and evaluation of <sup>68<\/sup>Ga\u2010 and <sup>153<\/sup>Sm\u2010labeled <scp>DOTA<\/scp>\u2010conjugated bisphosphonate ligand for potential use in detection of skeletal metastases and management of pain arising from skeletal metastases"],"prefix":"10.1111","volume":"92","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-8002-439X","authenticated-orcid":false,"given":"Sudipta","family":"Chakraborty","sequence":"first","affiliation":[{"name":"Radiopharmaceuticals Division Bhabha Atomic Research Centre (BARC)  Trombay, Mumbai Maharashtra India"},{"name":"Homi Bhabha National Institute  Anushakti Nagar, Mumbai Maharashtra India"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Dibakar","family":"Goswami","sequence":"additional","affiliation":[{"name":"Homi Bhabha National Institute  Anushakti Nagar, Mumbai Maharashtra India"},{"name":"Bio Organic Division Bhabha Atomic Research Centre (BARC)  Trombay, Mumbai Maharashtra India"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Rubel","family":"Chakravarty","sequence":"additional","affiliation":[{"name":"Radiopharmaceuticals Division Bhabha Atomic Research Centre (BARC)  Trombay, Mumbai Maharashtra India"},{"name":"Homi Bhabha National Institute  Anushakti Nagar, Mumbai Maharashtra India"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Sahiralam Khan","family":"Mohammed","sequence":"additional","affiliation":[{"name":"Radiopharmaceuticals Division Bhabha Atomic Research Centre (BARC)  Trombay, Mumbai Maharashtra India"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Haladhar Deb","family":"Sarma","sequence":"additional","affiliation":[{"name":"Radiation Biology and Health Sciences Division Bhabha Atomic Research Centre (BARC)  Trombay, Mumbai Maharashtra India"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ashutosh","family":"Dash","sequence":"additional","affiliation":[{"name":"Radiopharmaceuticals Division Bhabha Atomic Research Centre (BARC)  Trombay, Mumbai Maharashtra India"},{"name":"Homi Bhabha National Institute  Anushakti Nagar, Mumbai Maharashtra India"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2018,5,30]]},"reference":[{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.1002\/(SICI)1097-0142(19971015)80:8 <1588::AID-CNCR9>3.0.CO;2-G"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.3390\/ph10020045"},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0959-8049(97)10128-9"},{"key":"e_1_2_7_5_1","doi-asserted-by":"publisher","DOI":"10.1016\/8756-3282(95)00445-9"},{"key":"e_1_2_7_6_1","doi-asserted-by":"publisher","DOI":"10.1039\/b908652h"},{"key":"e_1_2_7_7_1","doi-asserted-by":"publisher","DOI":"10.1039\/B512310K"},{"key":"e_1_2_7_8_1","first-page":"559","volume":"64","author":"Fridell H.","year":"1950","journal-title":"Am. 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