Shyam K, Penketh P G, Loomis R H, Rose W C, Sartorelli A C
Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut 06520, USA.
J Med Chem. 1996 Feb 2;39(3):796-801. doi: 10.1021/jm9505021.
Several 2-(aminocarbonyl)-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydr azi nes were synthesized and primarily evaluated for antitumor activity against the murine L1210 leukemia. All of the compounds tested were capable of producing "cures" of mice bearing this tumor. One of the most active agents of this class, 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)- 2(-)[[2-chloroethyl)-amino]carbonyl]hydrazine, was further evaluated against a spectrum of transplanted murine and human solid tumors. Pronounced activity was found against all of the tumors including the murine B16F10 melanoma, M109 lung carcinoma, M5076 reticulum cell sarcoma, and the human LX-1 lung carcinoma. The activities observed compared favorably with those of the established antitumor drugs, cyclophosphamide, mitomycin C, and the nitrosoureas, evaluated concomitantly.
合成了几种2-(氨基甲酰基)-1,2-双(甲基磺酰基)-1-(2-氯乙基)肼，并对其抗小鼠L1210白血病的抗肿瘤活性进行了初步评估。所有测试的化合物都能够使携带这种肿瘤的小鼠“治愈”。该类中最具活性的药物之一，1,2-双(甲基磺酰基)-1-(2-氯乙基)-2-[[(2-氯乙基)-氨基]甲酰基]肼，进一步针对一系列移植的小鼠和人类实体瘤进行了评估。发现其对所有肿瘤都有显著活性，包括小鼠B16F10黑色素瘤、M109肺癌、M5076网状细胞肉瘤和人类LX-1肺癌。同时评估时，观察到的活性与已确立的抗肿瘤药物环磷酰胺、丝裂霉素C和亚硝基脲相比具有优势。
