916452-57-8Relevant articles and documents
Synthesis of 15,20-triamide analogue with polar substituent on the phenyl ring of arenastatin A, an extremely potent cytotoxic spongean depsipeptide
Kotoku, Naoyuki,Kato, Tomoya,Narumi, Fuminori,Ohtani, Emiko,Kamada, Sayo,Aoki, Shunji,Okada, Naoki,Nakagawa, Shinsaku,Kobayashi, Motomasa
, p. 7446 - 7457 (2007/10/03)
In order to increase metabolic stability and water solubility of arenastatin A, an extremely potent cytotoxic depsipeptide from the Okinawan marine sponge of Dysidea arenaria, several 15,20-triamide analogues with a polar substituent on the phenyl ring were synthesized. The 15,20-triamide analogues with a polar substituent (24, 30, and 31) showed increased solubility to MeOH and stronger cytotoxicity against KB cells in comparison with the parental 15,20-triamide analogue (2). Furthermore, the diethylamine analogue (30) exhibited in vivo anti-tumor activity against subcutaneously implanted murine sarcoma.