Sosnovsky G, Lukszo J, Gravela E, Zuretti M F
J Med Chem. 1985 Sep;28(9):1350-4. doi: 10.1021/jm00147a041.
Phosphonic (4a,b) and phosphinic (5a-d) analogues of ornithine were synthesized and evaluated for their inhibitory activity against ornithine decarboxylase and against the lymphocytic leukemia P388. The title compounds possess a low degree of inhibition against rat liver ornithine decarboxylase as compared to alpha-(difluoromethyl)ornithine. Thus, compounds 4a and 5a inhibit by 40% the ornithine decarboxylase activity at a 5 mM concentration. The other derivatives are less potent. Compounds 4a, 4b, 5b, and 5d are inactive against P388 tumor in CD2F1 mice at doses of 50 and 150 mg/kg.
合成了鸟氨酸的膦酸（4a,b）和次膦酸（5a-d）类似物，并评估了它们对鸟氨酸脱羧酶和淋巴细胞白血病P388的抑制活性。与α-（二氟甲基）鸟氨酸相比，标题化合物对大鼠肝脏鸟氨酸脱羧酶的抑制程度较低。因此，化合物4a和5a在5 mM浓度下可抑制鸟氨酸脱羧酶活性40%。其他衍生物的活性较弱。化合物4a、4b、5b和5d在50和150 mg/kg剂量下对CD2F1小鼠的P388肿瘤无活性。
