Six methylol derivatives of nitrofurylvinylogues were prepared from their parent compounds with formaldehyde or paraformaldehyde in water or in organic solvents. Of these, antitumor effect on Ehrlich ascites carcinoma in mice was investigated. 2-Bis(hydroxymethyl)amino-4-[2-(5-nitro-2-furyl) vinyl] pyrimidine (D-ran-methylol) and 2-bis(hydroxymethyl)amino-4-[2-(5-nitro-2-furyl) vinyl] quinoline (2A-4Q-ran-methylol) were revealed to save mice completely from tumor death with the suitable dose intraperitoneally. These two compounds had small toxicities and administrations of 1, 000 mg. per kilo did not kill any mouse.
                                    在
水或有机溶剂中,用
甲醛或多
聚甲醛从其母体化合物制备了六种硝基
糠醛基
乙烯基醚的
甲醇衍
生物。研究了这些衍
生物对小鼠艾氏腹
水癌的抗肿瘤作用。结果表明,腹腔注射适当剂量的 2-双(羟甲基)
氨基-4-[2-(5-硝基-2-
呋喃基)
乙烯基]
嘧啶(D-ran-methylol)和 2-双(羟甲基)
氨基-4-[2-(5-硝基-2-
呋喃基)
乙烯基]
喹啉(2A-4Q-ran-methylol)可使小鼠完全免于肿瘤死亡。这两种化合物的毒性较小,每公斤 1,000 毫克的剂量不会导致任何小鼠死亡。