Motohashi N, Kurihara T, Satoh K, Sakagami H, Molnár J
Department of Medicinal Chemistry, Meiji College of Pharmacy, Tokyo, Japan.
Anticancer Res. 1997 Nov-Dec;17(6D):4403-6.
The structure and activity relationship of fifteen "half-mustard type" phenothiazines and related compounds were investigated. These compounds did not show any direct bactericidal activity, possibly due to the lack of radical generation activity. Pretreatment with phenothiazines significantly reduced the lethality of Escherichia coli GN2411 infection, possibly due to activation of the host defense mechanism. Higher concentrations of these compounds showed cytotoxic activity against several cultured tumor cell lines. However, no clear-cut relationship was established between biological activity and two dipole moments (mu g, mu e).
研究了十五种“半芥末型”吩噻嗪及其相关化合物的结构与活性关系。这些化合物未表现出任何直接杀菌活性，可能是由于缺乏自由基生成活性。吩噻嗪预处理显著降低了大肠杆菌GN2411感染的致死率，可能是由于宿主防御机制的激活。这些化合物的较高浓度对几种培养的肿瘤细胞系表现出细胞毒性活性。然而，在生物活性与两个偶极矩（μg，μe）之间未建立明确的关系。
