In vitro and in vivo growth inhibition and G sub(1) arrest in human cancer cell lines by diaminophenyladamantane derivatives

We describe the discovery of a novel series of anticancer adamantane derivatives which induce G sub(1) arrest in Colo 205 and HT 29 colon cancer cells. Seven adamantane derivatives were screened for their activity in vitro against 60 human cancer cell lines in the National Cancer Institute (NCI)'s Anticancer Drug Screen system. The relationships between structure and in vitro anticancer activity are discussed. 1,3-Bis(4-(4-amino-3-hydroxyphenoxy)phenyl)adamantane (1,3-DPA/OH/NH sub(2)) and 2,2-bis(4-(4-amino-3-hydroxyphenoxy)phenyl)adamantane (DPA) exhibited strong growth inhibitory on anticancer activities in vitro. The IC sub(50)s of 1,3-DPA/OH/NH sub(2) (NSC-706835) and DPA (NSC-706832) were found to be