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Structure-Activity Relationship and in Vivo Anti-Tumor Evaluations of Dictyoceratin-A and -C, Hypoxia-Selective Growth Inhibitors from Marine Sponge

Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka 565-0871, Japan
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Academic Editor: Orazio Taglialatela-Scafati
Mar. Drugs 2015, 13(12), 7419-7432; https://doi.org/10.3390/md13127074
Received: 2 October 2015 / Revised: 1 December 2015 / Accepted: 3 December 2015 / Published: 16 December 2015
Oral dictyoceratin-C (1) and A (2), hypoxia-selective growth inhibitors, showed potent in vivo antitumor effects in mice subcutaneously inoculated with sarcoma S180 cells. Structurally modified analogs were synthesized to assess the structure–activity relationship of the natural compounds 1 and 2 isolated from a marine sponge. Biological evaluation of these analogs showed that the exo-olefin and hydroxyl and methyl ester moieties were important for the hypoxia-selective growth inhibitory activities of 1 and 2. Thus far, only substitution of the methyl ester with propargyl amide in 1 was found to be effective for the synthesis of probe molecules for target identification. View Full-Text
Keywords: dictyoceratin-C; dictyoceratin-A; hypoxia-selective growth inhibitor; marine sponge; analog synthesis; structure-activity relationship; in vivo antitumor effect dictyoceratin-C; dictyoceratin-A; hypoxia-selective growth inhibitor; marine sponge; analog synthesis; structure-activity relationship; in vivo antitumor effect
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Sumii, Y.; Kotoku, N.; Fukuda, A.; Kawachi, T.; Arai, M.; Kobayashi, M. Structure-Activity Relationship and in Vivo Anti-Tumor Evaluations of Dictyoceratin-A and -C, Hypoxia-Selective Growth Inhibitors from Marine Sponge. Mar. Drugs 2015, 13, 7419-7432.

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