IN-VITRO CYTOTOXICITY AND DIFFERENTIAL CELLULAR-SENSITIVITY OF DERIVATIVES OF DIAMINO ACIDS .1. N-1-METHYL, N-1-ALLYL, N-1-(2-CHLOROETHYL) AND N-1-PROPARGYL UREAS

The in vitro, cytotoxicity and differential cellular sensitivity of a series of new N-1-methyl, N-1-allyl, N-1-2-chloroethyl and N-1-proparg yl urea derivatives of diamino acids were determined in the National C ancer Institute's primary antitumor drug screen. The compounds tested showed an in vitro anticancer. activity similar to commercialized nitr osoureas such as CCNU, BCNU, MeCCNU chlorozotocin, streptozotocin and PCNU. The alkylating moiety of the ureas seems to play a role in the g eneral selectivity of our compounds. The N-1-methyl and N-1-2-chloroet hyl urea derivatives are more selective for central nervous system cel l lines and the N-1-allyl urea derivatives are more selective for lung cancer cell lines. The N-1-propargyl ureas did not show any particula r selectivity in the 60 human cell lines tested.