HYDROPHOBICITY OF SEVERAL RHODIUM(II) CARBOXYLATES CORRELATED WITH THEIR BIOLOGIC ACTIVITY
HYDROPHOBICITY OF SEVERAL RHODIUM(II) CARBOXYLATES CORRELATED WITH THEIR BIOLOGIC ACTIVITY
复制标题
DOI：
10.1021/jm00217a016
复制
发表时间：
1977-01-01
影响因子：
7.3
通讯作者：
BEAR, JL
中科院分区：
文献类型：
--
作者：
HOWARD, RA;SHERWOOD, E;BEAR, JL
铑（II）羧酸盐在抗肿瘤活性和毒性方面有很大差异，这取决于羧酸基团（甲氧基乙酸酯、丙酸酯、丁酸酯等）的性质。涉案铑（II）羧酸盐的溶解度特性与这些化合物显示的抗肿瘤活性和毒性密切相关。在体外的肿瘤细胞吸附的Rh的量也与研究的Rh（II）化合物的分配系数。存活和毒性研究表明，戊酸铑（II）对埃利希腹水小鼠肿瘤株具有最高的治疗指数，并且还表明，延长羧酸酯R链超过戊酸酯会降低药物的治疗效果。
Rhodium(II) carboxylates differ greatly in antitumor activity and toxicity depending on the properties of the carboxylate group (methoxyacetate, propionate, butyrate, etc.) involved. The solubility characteristics of rhodium(II) carboxylates correlate well with the antitumor activity and toxicity that these compounds display. The amount of Rh adsorbed by tumor cells in vitro also correlates with the partition coefficient of the Rh(II) compounds studied. Survival and toxicity studies show Rh(II) pentanoate to possess the highest therapeutic index against the Ehrlich ascites mouse tumor strain and also show that lengthening the carboxylate R chain beyond the pentanoate reduces the drugs'' therapeutic efficacy.