Seventeen new compounds were synthesized from gambogic acid (GA) with the structural modification of C-32. The reaction steps included selective epoxidation, periodate oxidation, methylation, Jones oxidation, different conditions of esterification, amidation, etc. The structures of target compounds were confirmed by NMR, IR and MS/ESI techniques. Their antitumor activities were evaluated in vitro by MTT assay. The results showed that compounds 5, 7, 8 and 13 were more potent than GA to human hepatoma cells (HepG2) and colon carcinoma cells (HCT-116).
Zhang Shenglie
,
Li Qian
,
Zhang Lei
,
Sun Haopeng
,
You Qidong
. Synthesis and Bioevaluation of Gambogic Acid Derivatives as Antitumor Agents[J]. Chinese Journal of Organic Chemistry, 2012
, 32(08)
: 1450
-1458
.
DOI: 10.6023/cjoc201204018
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