Paper
Potential bioreductive alkylating agents. 7. Antitumor effects of phenyl-substituted 2-chloromethyl-3-phenyl-1,4-naphthoquinones.
Published Nov 1, 1976 · A. Lin, A. Sartorelli
Journal of medicinal chemistry
25
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0
Influential Citations
Abstract
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.
Para-substituted methoxyphenyl, chlorophenyl, and bromophenyl derivatives of 2-chloromethyl-3-phenyl-1,4-naphthoquinone show comparable antitumor activity against Sarcoma 180 ascites cells,
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