Potential bioreductive alkylating agents. 7. Antitumor effects of phenyl-substituted 2-chloromethyl-3-phenyl-1,4-naphthoquinones.
Functional groups such as nitro, chloro, bromo, and methoxy were introduced in the meta and para positions of the phenyl ring of the antineoplastic agent 2-chloromethyl-3-phenyl-1,4-naphthoquinone. Tests for tumor-inhibitory potency of these derivatives against Sarcoma 180 ascites cells in mice indicated that the para-substituted methoxyphenyl, chlorophenyl, and bromophenyl derivatives possessed antitumor activity comparable to that of the parent compound 2-chloromethyl-3-phenyl-1,4-naphthoquinone, whereas meta-substituted nitro and bromo derivatives were either inactive or only weakly active anticancer agents in this system.
D000477:Alkylating Agents / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000627:therapeutic use; D000818:Animals; D004334:Drug Administration Schedule; D051379:Mice; D008815:Mice, Inbred Strains; D009285:Naphthoquinones / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000627:therapeutic use; D012510:Sarcoma 180 / Q000188:drug therapy; D013329:Structure-Activity Relationship
D000477:Alkylating Agents; D009285:Naphthoquinones