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).

Research highlights
► Annexin V is the gold standard probe for imaging apoptosis.
► Unfavorable profiles of Annexin V make it difficult to apply in the clinic.
► A novel small-molecular probe DNSBA was designed as an alternative to Annexin V.
► DNSBA specifically and selectively detect apoptotic cancer cells at all stages.
► DNSBA is a potential SPECT and PET agent when labeled with radioiodine.