Macrocyclic ketone analogues of halichondrin B.
Structurally simplified macrocyclic ketone analogues of halichondrin B were prepared by total synthesis and found to retain the potent cell growth inhibitory activity in vitro, stability in mouse serum, and in vivo efficacy of the natural product.
Department of Medicinal Chemistry, Eisai Research Institute, 4 Corporate Drive, Andover, MA 01810, USA.
Wanjun
W
Zheng
Boris M
BM
Seletsky
Monica H
MH
Palme
Paul J
PJ
Lydon
Lori A
LA
Singer
Charles E
CE
Chase
Charles A
CA
Lemelin
Yongchun
Y
Shen
Heather
H
Davis
Lynda
L
Tremblay
Murray J
MJ
Towle
Kathleen A
KA
Salvato
Bruce F
BF
Wels
Kimberley K
KK
Aalfs
Yoshito
Y
Kishi
Bruce A
BA
Littlefield
Melvin J
MJ
Yu
D000818:Animals; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D004988:Ethers, Cyclic / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D005663:Furans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007659:Ketones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D047028:Macrocyclic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D018942:Macrolides; D051379:Mice; D008968:Molecular Conformation; D013329:Structure-Activity Relationship; D000095662:Polyether Polyketides
D004988:Ethers, Cyclic; D005663:Furans; D007659:Ketones; D047028:Macrocyclic Compounds; D018942:Macrolides; C070519:halichondrin B; D000095662:Polyether Polyketides; C490954:eribulin