Abstract: AIMTo find derivatives of P-methyl-goniotriol with more potent antitumor activities and lacking undesirable effects. METHODSEighty derivatives of P-methyl-goniotriol have been synthesized in nine steps from α-D-glucoheptonic-δ-lactone (2). Compound 2 reacted with acetone in the catalyzer, H₂SO₄ and anhydrous MgSO₄, and then reacted with 60% aqua HOAc, finally was oxidized by NaIO₄ at room temperature into aldehyde 3 in a yield of 71.3%. The aldehyde 3 reacted immediately with P-CH₃-PhMgBr giving mixture 4. The mixture 4 was oxidized by NaIO₄, reacted with Ph₃PCHCO₂Et and then induced by catalyzer. 1,8-Diazabicylclo［5,4,0］undec-7-ene in THF providing the compounds 6 and 7. The esterfication of 6 with cinnamyl chloride et al in 4-dimethylaminopyridine, Et₃N gave the esters 8a～h. Acid hydrolysis of the acetone protecting group of 8a～h in 75% aqua HOAc gave compounds 9a～h. Their chemical structures were confirmed by IR, 1HNMR, MS and element analysis. The antitumor activities of the compounds were screened by MTT methods. RESULTSFifteen derivatives of P-methyl-goniotriol (7, 8b～h, 9b～h) are new compounds. CONCLUSIONPharmacological tests indicate that these compounds showed antitumor activities toward tumor cells (A2780, HCT-8, Bel742, KB) in vitro. The antitumor activities of 8b, 8d, 8g and 9h were more potent than howiinol A.