Breccia A, Busi F, Gattavecchia E, Tamba M
Istituto di Scienze Chimiche, Università di Bologna, Italy.
Radiat Environ Biophys. 1990;29(3):153-60. doi: 10.1007/BF01210519.
A new series of nitrothiophene derivatives have been synthetized and some of the physico-chemical parameters which can influence both their radiosensitizing efficiency and toxicity have been investigated. These include octanol/water partition coefficient (P), one-electron reduction potential (E7(1] and reactivity of the drugs towards primary radical species. For these studies, pulse radiolysis techniques and conventional polarography have been extensively used. Biological responses (both sensitization and toxicity) have been tested towards Chinese Hamster cells in vitro. The results are valuable in selecting, among the tested compounds, 5-NTMA, 5-NTM, 4- and 5-NTCA as the nitrohiophenes promising for in vivo applications.
已合成了一系列新的硝基噻吩衍生物,并研究了一些可能影响其放射增敏效率和毒性的物理化学参数。这些参数包括辛醇/水分配系数(P)、单电子还原电位(E1/2)以及药物对初级自由基的反应性。在这些研究中,脉冲辐解技术和传统极谱法得到了广泛应用。已在体外对中国仓鼠细胞测试了生物反应(包括增敏和毒性)。这些结果对于在测试化合物中选择5-NTMA、5-NTM、4-和5-NTCA作为有望用于体内应用的硝基噻吩具有重要价值。