Synthesis, characterization, and radioprotective activity of α,β-unsaturated aryl sulfone analogs and their Tempol
Nan Zhou1, Tian Feng1, Xin Shen1
1Department of Medicinal Chemistry , School of Pharmacy , Fourth Military Medical University , Xi'an 710032 , Shaanxi , China . Email: syzhang@fmmu.edu.cn ;
Abstract:
Some novel α,β-unsaturated aromatic sulfone analogs (5a-5m) and their Tempol conjugates (6a-6e) have been synthetically prepared, characterized and evaluated for their radioprotective activity under γ-ray radiation. The Tempol conjugates were characterized by X-ray single crystal diffraction. In vitro studies showed that 5a, 5b and 6b had superior activities to Ex-Rad pre-treated before 5 Gy irradiation, and 5a, 6a and 6b had better activities than Ex-Rad after 5 Gy irradiation, while 5a, 6a and 6b exhibited both prophylactic and mitigation effects, indicating the advantage of combining α,β-unsaturated aromatic sulfones with Tempol nitroxide. Both p53 and phospho-p53 levels were significantly lower in compound-treated cells than those in untreated irradiated cells. The conjugates offer an improved radioprotective ability, which is an advantage in the treatment protocol.
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