Literature DB >> 19691348

Discovery of [18F]N-(2-(diethylamino)ethyl)-6-fluoronicotinamide: a melanoma positron emission tomography imaging radiotracer with high tumor to body contrast ratio and rapid renal clearance.

Ivan Greguric1, Stephen R Taylor, Delphine Denoyer, Patrice Ballantyne, Paula Berghofer, Peter Roselt, Tien Q Pham, Filomena Mattner, Thomas Bourdier, Oliver C Neels, Donna S Dorow, Christian Loc'h, Rodney J Hicks, Andrew Katsifis.   

Abstract

The high melanoma uptake and rapid body clearance displayed by our series of [(123)I]iodonicotinamides prompted the development of [(18)F]N-(2-(diethylamino)ethyl)-6-fluoronicotinamide ([(18)F]2), a novel radiotracer for PET melanoma imaging. Significantly, unlike fluorobenzoates, [(18)F]fluorine incorporation on the nicotinamide ring is one step, facile, and high yielding. [(18)F]2 displayed high tumor uptake, rapid body clearance via predominantly renal excretion, and is currently being evaluated in preclinical studies for progression into clinical trials to assess the responsiveness of therapeutic agents.

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Year:  2009        PMID: 19691348     DOI: 10.1021/jm9008423

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  12 in total

Review 1.  PET and SPECT imaging of melanoma: the state of the art.

Authors:  Weijun Wei; Emily B Ehlerding; Xiaoli Lan; Quanyong Luo; Weibo Cai
Journal:  Eur J Nucl Med Mol Imaging       Date:  2017-10-30       Impact factor: 9.236

2.  The [F]2-Fluoro-1,3-thiazolyl Moiety - an Easily-Accessible Structural Motif for Prospective Molecular Imaging Radiotracers.

Authors:  Fabrice G Siméon; Matthew T Wendahl; Victor W Pike
Journal:  Tetrahedron Lett       Date:  2010-11-17       Impact factor: 2.415

3.  Early detection and longitudinal monitoring of experimental primary and disseminated melanoma using [¹⁰F]ICF01006, a highly promising melanoma PET tracer.

Authors:  Latifa Rbah-Vidal; Aurélien Vidal; Sophie Besse; Florent Cachin; Mathilde Bonnet; Laurent Audin; Serge Askienazy; Frédéric Dollé; Françoise Degoul; Elisabeth Miot-Noirault; Nicole Moins; Philippe Auzeloux; Jean-Michel Chezal
Journal:  Eur J Nucl Med Mol Imaging       Date:  2012-06-16       Impact factor: 9.236

Review 4.  MC1R and melanin-based molecular probes for theranostic of melanoma and beyond.

Authors:  Hui Shi; Zhen Cheng
Journal:  Acta Pharmacol Sin       Date:  2022-08-25       Impact factor: 7.169

5.  A novel aliphatic 18F-labeled probe for PET imaging of melanoma.

Authors:  Hongguang Liu; Shuanglong Liu; Zheng Miao; Han Jiang; Zixin Deng; Xuechuan Hong; Zhen Cheng
Journal:  Mol Pharm       Date:  2013-08-22       Impact factor: 4.939

6.  Imaging malignant melanoma with (18)F-5-FPN.

Authors:  Hongyan Feng; Xiaotian Xia; Chongjiao Li; Yiling Song; Chunxia Qin; Qingyao Liu; Yongxue Zhang; Xiaoli Lan
Journal:  Eur J Nucl Med Mol Imaging       Date:  2015-08-11       Impact factor: 9.236

7.  Development of 18F-labeled picolinamide probes for PET imaging of malignant melanoma.

Authors:  Hongguang Liu; Shuanglong Liu; Zheng Miao; Zixin Deng; Baozhong Shen; Xuechuan Hong; Zhen Cheng
Journal:  J Med Chem       Date:  2013-01-18       Impact factor: 7.446

8.  Synthesis and preclinical characterization of [18F]FPBZA: a novel PET probe for melanoma.

Authors:  Shih-Yen Wu; Shih-Pin Huang; Yen-Chen Lo; Ren-Shyan Liu; Shyh-Jen Wang; Wuu-Jyh Lin; Chih-Chieh Shen; Hsin-Ell Wang
Journal:  Biomed Res Int       Date:  2014-09-01       Impact factor: 3.411

9.  Selective targeting of melanoma using N-(2-diethylaminoethyl) 4-[18F]fluoroethoxy benzamide (4-[18F]FEBZA): a novel PET imaging probe.

Authors:  Pradeep K Garg; Rachid Nazih; Yanjun Wu; Vladimir P Grinevich; Sudha Garg
Journal:  EJNMMI Res       Date:  2017-08-08       Impact factor: 3.138

10.  Ultrasensitive detection of malignant melanoma using PET molecular imaging probes.

Authors:  Ayoung Pyo; Dong-Yeon Kim; Heejung Kim; Daejin Lim; Seong Young Kwon; Sae-Ryung Kang; Hyung-Seok Kim; Hee-Seung Bom; Jung-Joon Min
Journal:  Proc Natl Acad Sci U S A       Date:  2020-05-21       Impact factor: 11.205

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