Several natural guaianolides and synthetic derivatives of repin (1) were tested and found to be active against tumor cell replication. Repin (1) and both mono- and di-halohydrin analogues (2, 7-9, 11, 12) showed significant antitumor potency. A more effective compound (17) was obtained by esterificating repin with the paclitaxel side chain.
Several natural and synthetic sesquiterpene lactones with different skeletons were tested and found to be active against nine cancer cell lines. Elemane, heliangolane and their hydroxy analogues 9 and 10, all containing an alpha,beta-unsaturated aldehyde substituent, were the most potent compounds.
A study on the acid‐induced rearrangement of 4,5‐epoxy‐ and 1,10‐epoxygermacra‐8,12‐olides was carried out. From a 4,5‐epoxy derivative, guaianes were obtained, whereas 1,10‐epoxy derivatives furnished, depending on the stereochemistry of the C‐1/C‐10 epoxy ring, trans‐5β,10α‐ or trans‐5α,10β‐eudesmanolides.
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