Motohashi N, Kurihara T, Sakagami H, Szabo D, Csuri K, Molnár J
Department of Medicinal Chemistry, Meiji Pharmaceutical University, Tokyo, Japan.
Anticancer Res. 1999 May-Jun;19(3A):1859-64.
The antiproliferative activity of six "half-mustard type" phenothiazines against a total of 54 tumor cell lines: 4 leukemia, 9 non-small-cell lung, 7 colon-, 5 CNS-, 8 melanoma, 6 ovarian-, 8 renal-, 1 prostate and 6 breast cancer was determined by NCI-Information Intensive-Approach. The C-2 position of phenothiazines were substituted with H, Cl and CF3 groups. The half-mustard and ring system was linked either by a propylene or a butylene bridge. Colon-cancer cell showed the highest sensitivity against "half-mustard type" phenothiazines, followed by leukemia, melanoma, prostate-, CNS-, breast-, lung-, renal and ovarian cancer cells. These data suggest the "cancer-type-specific" antitumor action of "half-mustard type" phenothiazines.
采用美国国立癌症研究所（NCI）信息密集型方法，测定了六种“半芥子型”吩噻嗪对总共54种肿瘤细胞系的抗增殖活性，这些细胞系包括4种白血病细胞系、9种非小细胞肺癌细胞系、7种结肠癌细胞系、5种中枢神经系统癌细胞系、8种黑色素瘤细胞系、6种卵巢癌细胞系、8种肾癌细胞系、1种前列腺癌细胞系和6种乳腺癌细胞系。吩噻嗪的C-2位被氢、氯和三氟甲基取代。半芥子基团与环系统通过丙烯桥或丁烯桥相连。结肠癌细胞对“半芥子型”吩噻嗪表现出最高的敏感性，其次是白血病、黑色素瘤、前列腺癌、中枢神经系统癌、乳腺癌、肺癌、肾癌和卵巢癌细胞。这些数据表明“半芥子型”吩噻嗪具有“癌症类型特异性”抗肿瘤作用。
