Neil G L, Kuentzel S L, McGovren J P
Cancer Treat Rep. 1979 Nov-Dec;63(11-12):1971-8.
The chemotherapeutic activity of analogs of the anthracycline antibiotic, nogalamycin, was investigated in the P388 and L1210 leukemias and the B16 melanoma in mice. Among the compounds tested, 7-con-O-methylnogarol was found to have superior activity. Depending on the route and schedule of administration, increases in lifespan (ILS) in excess of 100% were observed in all three tumor systems. Additional testing of 7-con-O-methylnogarol demonstrated significant activity in the murine colon 26 and colon 38 tumors and the CD8F1 mammary tumor. 7-Con-O-methylnogarol was not significantly effective against murine Lewis lung carcinoma, although ILSs of 38% and 29% were achieved in two experiments. Activity was observed against ip inoculated P388 leukemia after ip, sc, oral, and iv drug administration. 7-Con-O-methylnogarol was also highly active (ILS greater than or equal to 120%) after ip drug administration to mice with iv inoculated P388 leukemia. Significant ILS values resulted from a variety of schedules of administration against ip inoculated P388 leukemia and B16 melanoma. Experiments in which the time of single-dose administration was varied prior to the time of ip P388 leukemia inoculation showed that residual drug or bioactive drug-related materials remained in mice for 8 hours after 50 mg/kg administered ip and for 48 hours after 200 mg/kg administered sc.
研究了蒽环类抗生素诺加霉素类似物在小鼠P388和L1210白血病以及B16黑色素瘤中的化疗活性。在所测试的化合物中，发现7-顺式-O-甲基诺加罗具有更高的活性。根据给药途径和方案，在所有三个肿瘤系统中均观察到寿命延长（ILS）超过100%。对7-顺式-O-甲基诺加罗的进一步测试表明，其在小鼠结肠26和结肠38肿瘤以及CD8F1乳腺肿瘤中具有显著活性。7-顺式-O-甲基诺加罗对小鼠Lewis肺癌没有显著疗效，尽管在两项实验中分别实现了38%和29%的ILS。在腹腔注射、皮下注射、口服和静脉注射给药后，观察到对腹腔接种的P388白血病有活性。对静脉接种P388白血病的小鼠腹腔注射药物后，7-顺式-O-甲基诺加罗也具有高活性（ILS大于或等于120%）。针对腹腔接种的P388白血病和B16黑色素瘤，多种给药方案产生了显著的ILS值。在腹腔接种P388白血病之前改变单剂量给药时间的实验表明，腹腔注射50mg/kg后，小鼠体内残留药物或生物活性药物相关物质持续8小时，皮下注射200mg/kg后持续48小时。
