Syntheses and biological evaluation of C-3′-N-acyl modified taxane analogues from 1-deoxybaccatin-VI

• A series of taxane derivatives with three hydroxyl groups were synthesized.
• Several compounds showed excellent cytotoxicity against MBA-MB-231 and PC-3.
• Compounds 13a and 13d are more potent than Paclitaxel against HepG2 and H460.
• Compound 13d was most active in all series.
• Compound 18 was more active than compound 20 against MDA-MB-231 and PC-3.

A series of side-chain modified taxane analogues were synthesized and their in vitro anticancer activities against four human cancer cell lines: MDA-MB-231 (human breast cancer), PC-3 (human prostatic cancer), HepG2 and H460 (human hepatoma) were studied. The three hydroxyl groups at C-7, C-9 and C-10 enable the behavior of these compounds to be evidently distinct from other similar compounds. The strong cytotoxicity in the four cell lines showed by the newly synthesized taxane analogues 13a and 13d indicated them as potential lead compounds for anticancer drug design.

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