Wallace R E, Murdock K C, Angier R B, Durr F E
Cancer Res. 1979 May;39(5):1570-4.
1,4-Dihydroxy-5,8-bis(((2[(2-hydroxyethyl)amino]ethyl)amino))-9,-10-anthracenedione dihydrochloride (CL 232315; NSC 301739D), a representative of a new chemical class of compounds with antineoplastic properties, has been evaluated for antitumor activity in experimental mouse tumor systems. The compound produced significant increases in life span (ILS) and long-term survivors when tested against the P388 and L1210 leukemias as well as the solid neoplasms, B16 melanoma and Colon Tumor 26. The optimal treatment regimens resulted in a 173 to greater than 200% ILS with 20 to 80% 60-day survivors in mice with P388 leukemia, A 205% ILS with 55% 60-day survivors in mice with L1210 leukemia, and an ILS of greater than 300% with 80% 90-day survivors in mice with B16 melanoma. In contrast to Adriamycin, CL 232315 was active against the i.v. implanted L1210 leukemia and demonstrated moderate activity against P388/Adria, a subline of P388 resistant to Adriamycin. The compound was ineffective when tested against the Lewis lung carcinoma and the Ridgway osteogenic sarcoma. CL 232315 was active i.p., s.c., and i.v., but p.o. activity was not demonstrated. Schedule dependency was not observed when the compound was administered once daily for nine days, once every four days, or as a single dose.
1,4 - 二羟基 - 5,8 - 双(((2 - [(2 - 羟乙基)氨基]乙基)氨基)) - 9,10 - 蒽二酮二盐酸盐(CL 232315;NSC 301739D)是一类具有抗肿瘤特性的新型化合物的代表,已在实验小鼠肿瘤系统中评估其抗肿瘤活性。该化合物在针对P388和L1210白血病以及实体瘤B16黑色素瘤和结肠癌26进行测试时,显著延长了生存期(ILS)并产生了长期存活者。最佳治疗方案使P388白血病小鼠的ILS提高了173%至超过200%,60天存活者为20%至80%;L1210白血病小鼠的ILS为205%,60天存活者为55%;B16黑色素瘤小鼠的ILS大于300%,90天存活者为80%。与阿霉素不同,CL 232315对静脉注射植入的L1210白血病有活性,并对P388/Adria(P388对阿霉素耐药的亚系)表现出中等活性。该化合物在针对刘易斯肺癌和里奇韦骨肉瘤进行测试时无效。CL 232315腹腔注射、皮下注射和静脉注射均有活性,但口服无活性。当该化合物每天给药一次,连续九天,每四天给药一次或单次给药时,未观察到给药方案依赖性。