Antitumor Activity of Tetrahydroisoquinoline Analogues 3-epi-Jorumycin and 3-epi-Renieramycin G

摘要

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 GI50 values in the low nanomolar range (1.9–24.3 nM), while compounds >2–>4 were found to be substantially less cytotoxic (GI50 0.6–14.0 µM).