Antitumor activity of tetrahydroisoquinoline analogues 3- epi-jorumycin and 3- epi-renieramycin G

Analogues of the tetrahydroisoquinoline family of antitumor antibiotics, 3- epi-jorumycin ( 3) and 3- epi-renieramycin G ( 4), in addition to their respective parent natural products (−)-jorumycin ( 1) and (−)-renieramycin G ( 2) were evaluated against both human colon (HCT-116) and human lung (A549...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2006-06, Vol.16 (12), p.3180-3183
Hauptverfasser: Lane, Jonathan W., Estevez, Alberto, Mortara, Kyle, Callan, Ondine, Spencer, Jeffrey R., Williams, Robert M.
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Sprache:eng
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Zusammenfassung:Analogues of the tetrahydroisoquinoline family of antitumor antibiotics, 3- epi-jorumycin ( 3) and 3- epi-renieramycin G ( 4), in addition to their respective parent natural products (−)-jorumycin ( 1) and (−)-renieramycin G ( 2) were evaluated against both human colon (HCT-116) and human lung (A549) cancer cell lines. (−)-Jorumycin ( 1) displayed potent growth inhibition with GI 50 values in the low nanomolar range (1.9–24.3 nM), while compounds 2– 4 were found to be substantially less cytotoxic (GI 50 0.6–14.0 μM).
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.03.042