New antineoplastic aza-phospholipids - synthesis, in-vitro cytotoxicity and differential cellular-sensitivity against...

The in vitro cytotoxicity and differential cellular sensitivity of three new synthetic anti-neoplastic aza-phospholipids has been determined in the National Cancer Institute's (NCI) primary antitumor drug screen. Based on a disease-oriented strategy, this screen incorporates seventy human cell lines representing leukemia, ovarian, brain, melanoma, colon, renal, lung, prostate and breast cancers. The analysis of the GI50 values obtained for each aza-derivative has revealed a differential cellular sensitivity among the cell lines examined. The study of the degree of differential growth inhibition has shown a statistically significant differential cell sensitivity for BN 52205 and BN 52211 for colon and melanoma tumor cells. The leukemia cell selectivity for BN 52211 was even more remarkable due to the low molar concentration at which the maximum selective effect occurred. These findings strongly encourage further investigations on the anti-neoplastic activity of aza-phospholipids.