Design, synthesis, and biological evaluation of 4-(5-dimethylamino-naphthalene-1-sulfon-amido)-3-(4-iodophenyl)butanoic acid as a novel molecular probe for apoptosis imaging.
Apoptosis (programmed cell death) plays a crucial role in the pathogenesis of many disorders, thus the detection of apoptotic cells can provide the physician with important information to further therapeutic strategies and would substantially advance patient care. A small molecule, 4-(5-dimethylamino-naphthalene-1-sulfonamido)-3-(4-iodo-phenyl)butanoic acid (DNSBA), was designed as a novel probe for imaging apoptosis and synthesized with good yield. The biological characterization demonstrated that DNSBA can be used to specifically and selectively detect apoptotic cancer cells at all stages. DNSBA is also designed as a potential SPECT and PET probe when labeled with radioiodine (I-123, -124, and -131).
Zeng
Wenbin
W
School of Pharmaceutical Sciences, Central South University, 172 Tongzipo Road, Changsha 410078, China. wbzeng@hotmail.com
Miao
Weimin
W
Le Puil
Michael
M
Shi
Guangqing
G
Biggerstaff
John
J
Kabalka
George W
GW
Townsend
David
D
D017209:Apoptosis; D045744:Cell Line, Tumor; D003619:Dansyl Compounds / Q000138:chemical synthesis / Q000737:chemistry*; D005456:Fluorescent Dyes / Q000138:chemical synthesis / Q000737:chemistry*; D006801:Humans; D009369:Neoplasms / Q000473:pathology*; D010666:Phenylpropionates / Q000138:chemical synthesis / Q000737:chemistry*; D049268:Positron-Emission Tomography / Q000379:methods
C551923:4-(5-dimethylaminonaphthalene-1-sulfonamido)-3-(4-iodophenyl)butanoic acid; D003619:Dansyl Compounds; D005456:Fluorescent Dyes; D010666:Phenylpropionates