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M J Towle, K A Salvato, J Budrow, B F Wels, G Kuznetsov, K K Aalfs, S Welsh, W Zheng, B M Seletsky, M H Palme, G J Habgood, L A Singer, L V Dipietro, Y Wang, J J Chen, D A Quincy, A Davis, K Yoshimatsu, Y Kishi, M J Yu, B A Littlefield
Halichondrin B is a highly potent anticancer agent originally found in marine sponges. Although scarcity of the natural product has hampered efforts to develop halichondrin B as a new anticancer drug, the existence of a complete synthetic route has allowed synthesis of structurally simpler analogues that retain the remarkable potency of the parent compound. In this study, we show that two macrocyclic ketone analogues of halichondrir B, ER-076349 and ER-086526, have sub-nM growth inhibitory activities in vitro against numerous human cancer cell lines as well as marked in vivo activities at 0...
February 1, 2001: Cancer Research
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