Abstract:
:Lactimidomycin (LTM, 1), iso-migrastatin (iso-MGS, 2) and migrastatin (MGS, 3) are macrolide antitumor antibiotics differing in macrolide ring size but all bearing a glutarimide side chain. To further develop these natural products and related analogs as drug candidates we have produced and evaluated the biological activities of a small library of iso-MGS and LTM-derived agents; congeners evaluated bear either the MGS scaffold or related acyclic (dorrigocin) scaffolds. Scratch wound-healing (SWH) assays with 4T1 mouse and MDA-MB-231 human mammary tumor cell lines, respectively, reveal structural elements crucial to inhibition of cell migration by these compounds. Moreover, two substances, 14 and 17, with activity far superior to that of MGS are unveiled by SWH assays.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Ju J,Rajski SR,Lim SK,Seo JW,Peters NR,Hoffmann FM,Shen Bdoi
10.1016/j.bmcl.2008.07.072subject
Has Abstractpub_date
2008-11-15 00:00:00pages
5951-4issue
22eissn
0960-894Xissn
1464-3405pii
S0960-894X(08)00851-2journal_volume
18pub_type
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