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Synthesis and Characterization of Nitroimidazole Derivatives for (68)Ga-Labeling and Testing in Tumor Xenografted Mice

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dc.contributor.authorHoigebazar, Lathika-
dc.contributor.authorJeong, Jae Min-
dc.contributor.authorChoi, Soo Young-
dc.contributor.authorChoi, Jae Yeon-
dc.contributor.authorLee, Yun-Sang-
dc.contributor.authorChung, June-Key-
dc.contributor.authorChung, Young Keun-
dc.contributor.authorLee, Myung Chul-
dc.contributor.authorLee, Dong Soo-
dc.contributor.authorShetty, Dinesh-
dc.date.accessioned2012-07-03T07:39:07Z-
dc.date.available2012-07-03T07:39:07Z-
dc.date.issued2010-09-09-
dc.identifier.citationJOURNAL OF MEDICINAL CHEMISTRY; Vol.53 17; 6378-6385ko_KR
dc.identifier.issn0022-2623-
dc.identifier.urihttps://hdl.handle.net/10371/78292-
dc.description.abstractRadiolabeled nitroimidazole (NI) derivatives have been used for imaging hypoxic tissues. We synthesized NI derivatives conjugated with bifunctional chelating agents such as 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA) and isothiocyanatobenzyl-NOTA (SCN-NOTA) via ethyleneamine bridge by formation of amide and thiourea bond, respectively. We proved that amide oxygen of Ga-NOTA-NI contributes to the formation of metal complex by X-ray crystallography. We labeled them with (68)Ga and found that both (68)Ga-NOTA-NI and (68)Ga- SCN-NOTA-NI were labeled in high efficiency (> 96%) and were stable at room temperature in the prepared medium and at 37 degrees C in human serum. In vitro cell uptake experiments using CHO and CT-26 cell lines showed significantly increased uptakes of both of the agents in hypoxic condition. Biodistribution study in CT-26 xenografted mice showed increasing tumor to muscle ratios. (68)Ga-NOTA-NI showed lower intestine uptake than (68)Ga-NOTA-SCN-NI due to hydrophilicity. Also, (68)Ga-NOTA-NI showed higher tumor uptake than (68)Ga-NOTA-SCN-NI in an animal PET study. In conclusion, we successfully developed (68)Ga labeled NI derivatives for hypoxic tissue imaging.ko_KR
dc.description.sponsorshipThis work was supported by NRF of
Korea (Grants R0A-2008-000-20116-0 and 2009-0082087),
funded by Ministry of Education, Science and Technology.		ko_KR
dc.language.isoenko_KR
dc.publisherAMER CHEMICAL SOCko_KR
dc.titleSynthesis and Characterization of Nitroimidazole Derivatives for (68)Ga-Labeling and Testing in Tumor Xenografted Miceko_KR
dc.typeArticleko_KR
dc.contributor.AlternativeAuthor정재민-
dc.contributor.AlternativeAuthor최수영-
dc.contributor.AlternativeAuthor최재연-
dc.contributor.AlternativeAuthor이윤상-
dc.contributor.AlternativeAuthor이동수-
dc.contributor.AlternativeAuthor정준기-
dc.contributor.AlternativeAuthor이명철-
dc.contributor.AlternativeAuthor정영근-
dc.identifier.doi10.1021/jm100545a-
dc.citation.journaltitleJOURNAL OF MEDICINAL CHEMISTRY-
dc.description.citedreferenceYang BY, 2010, NUCL MED BIOL, V37, P149, DOI 10.1016/j.nucmedbio.2009.10.010-
dc.description.citedreferencePostema EJ, 2009, EUR J NUCL MED MOL I, V36, P1565, DOI 10.1007/s00259-009-1154-5-
dc.description.citedreferenceLiu RS, 2009, NUCL MED BIOL, V36, P305, DOI 10.1016/j.nucmedbio.2008.12.011-
dc.description.citedreferenceJEONG JM, 2009, NUCL MED MOL IMAGING, V43, P330-
dc.description.citedreferenceKomar G, 2008, J NUCL MED, V49, P1944, DOI 10.2967/jnumed.108.053785-
dc.description.citedreferenceRiss PJ, 2008, BIOORG MED CHEM LETT, V18, P5364, DOI 10.1016/j.bmcl.2008.09.054-
dc.description.citedreferenceMallia MB, 2008, BIOORG MED CHEM LETT, V18, P5233, DOI 10.1016/j.bmcl.2008.08.069-
dc.description.citedreferenceLewis JS, 2008, J NUCL MED, V49, P1177, DOI 10.2967/jnumed.108.051326-
dc.description.citedreferenceJeong JM, 2008, J NUCL MED, V49, P830, DOI 10.2967/jnumed.107.047423-
dc.description.citedreferenceTakasawa M, 2008, STROKE, V39, P1629, DOI 10.1161/STROKEAHA.107.485938-
dc.description.citedreferenceBussink J, 2008, INT J RADIAT ONCOL, V70, P1616, DOI 10.1016/j.ijrobp.2007.11.052-
dc.description.citedreferenceLucignani G, 2008, EUR J NUCL MED MOL I, V35, P838, DOI 10.1007/s00259-008-0740-2-
dc.description.citedreferenceVelikyan I, 2008, BIOCONJUGATE CHEM, V19, P569, DOI 10.1021/bc700341x-
dc.description.citedreferenceLee ST, 2007, SEMIN NUCL MED, V37, P451, DOI 10.1053/j.semnuclmed.2007.07.00.1-
dc.description.citedreferenceGrosu AL, 2007, INT J RADIAT ONCOL, V69, P541, DOI 10.1016/j.ijrobp.2007.05.079-
dc.description.citedreferenceSouvatzoglou M, 2007, EUR J NUCL MED MOL I, V34, P1566, DOI 10.1007/s00259-007-0424-3-
dc.description.citedreferenceOswald J, 2007, CANCER LETT, V254, P102, DOI 10.1016/j.canlet.2007.02.016-
dc.description.citedreferenceBreeman WAP, 2007, EUR J NUCL MED MOL I, V34, P978, DOI 10.1007/s00259-007-0387-4-
dc.description.citedreferenceReischl G, 2007, J PHARM PHARM SCI, V10, P203-
dc.description.citedreferenceYapp DTT, 2007, BJU INT, V99, P1154, DOI 10.1111/j.1464-410X.2007.06761.x-
dc.description.citedreferenceVVERE A, 2007, DALTON T, P4893-
dc.description.citedreferenceRajendran JG, 2006, CLIN CANCER RES, V12, P5435, DOI 10.1158/1078-0432.CCR-05-1773-
dc.description.citedreferenceRajendran JG, 2006, EUR J NUCL MED MOL I, V33, pS44, DOI 10.1007/s00259-006-0135-1-
dc.description.citedreferenceReischl G, 2005, APPL RADIAT ISOTOPES, V62, P897, DOI 10.1016/j.apradiso.2004.12.004-
dc.description.citedreferencePiert M, 2005, J NUCL MED, V46, P106-
dc.description.citedreferenceMAECKE HR, 2005, J NUCL MED, V46, P172-
dc.description.citedreferenceBarthel H, 2004, BRIT J CANCER, V90, P2232, DOI 10.1038/sj.bjc.6601862-
dc.description.citedreferenceGronroos T, 2004, EUR J NUCL MED MOL I, V31, P513, DOI 10.1007/s00259-003-1404-x-
dc.description.citedreferenceSorger D, 2003, NUCL MED BIOL, V30, P317, DOI 10.1016/S0969-8051(02)00442-0-
dc.description.citedreferenceZiemer LS, 2003, EUR J NUCL MED MOL I, V30, P259, DOI 10.1007/s00259-002-1037-5-
dc.description.citedreferenceZhang XG, 2001, NUCL MED BIOL, V28, P949-
dc.description.citedreferenceRiche F, 2001, BIOORG MED CHEM LETT, V11, P71-
dc.description.citedreferenceDolbier WR, 2001, APPL RADIAT ISOTOPES, V54, P73-
dc.description.citedreferencePrata MIM, 2000, J INORG BIOCHEM, V79, P359-
dc.description.citedreferenceMelo T, 2000, J NUCL MED, V41, P169-
dc.description.citedreferenceLewis JS, 1999, J NUCL MED, V40, P177-
dc.description.citedreferenceRauth AM, 1998, INT J RADIAT ONCOL, V42, P755-
dc.description.citedreferenceAndre JP, 1998, CHEM COMMUN, P1301-
dc.description.citedreferenceTewson TJ, 1997, NUCL MED BIOL, V24, P755-
dc.description.citedreferenceWu CC, 1997, BIOCONJUGATE CHEM, V8, P365-
dc.description.citedreferenceOtwinowski Z, 1997, METHOD ENZYMOL, V276, P307-
dc.description.citedreferenceSHELDRICK GM, 1997, SHELXS97 SHELXL97-
dc.description.citedreferenceSHI CQX, 1995, J NUCL MED, V36, P1078-
dc.description.citedreferenceYANG DJ, 1995, RADIOLOGY, V194, P795-
dc.description.citedreferenceNUNN A, 1995, EUR J NUCL MED, V22, P265-
dc.description.citedreferenceNORMAN TJ, 1995, SUPRAMOL CHEM, V4, P305-
dc.description.citedreferenceMARTIN GV, 1992, J NUCL MED, V33, P2202-
dc.description.citedreferenceJYO A, 1990, ANAL SCI, V6, P323-
dc.description.citedreferenceCRAIG AS, 1989, J CHEM SOC CHEM COMM, P1793-
dc.description.citedreferenceSHELTON ME, 1989, J NUCL MED, V30, P351-
dc.description.citedreferenceMARTIN GV, 1989, J NUCL MED, V30, P194-
dc.description.citedreferenceJOHNSON C, 1976, ORNL5138, P1718-
dc.description.tc10-
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