Structure-function relationships of alkyl-lysophospholipid analogs in selective antitumor activity.
Structure-function relationships of alkyl-lysophospholipid analogs in selective antitumor activity.
复制标题
烷基溶血磷脂类似物在选择性抗肿瘤活性中的结构-功能关系。
作者：
Vogler,WR;Olson,AC;Hajdu,J;Shoji,M;Raynor,R;Kuo,JF
This investigation was initiated in order to delineate the structure-function relationship of the anticancer alkyllysophospholipids and assess their degree of selective cytotoxicity toward neoplastic cells. A series of glycerol phosphocholine analogs with varying substitutions in thesn-1 andsn-2 position were tested for their inhibitory activity as measured by thymidine incorporation, clonogenic assays and effects on protein kinase C activity against a series of human leukemic cell lines and healthy bone marrow progenitor cells. The IC50was determined for each of the compounds in each cell line and healthy bone marrow cells following a 4-h incubation. The data indicated that a 16–18 carbon chain at thesn-1 coupled with a short substitution atsn-2 had the broadest antitumor activity and was the least toxic to normal bone marrow cells. The results provide a number of useful leads toward the design and development of potentially more active phospholipid compounds.
