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To improve the biological anticancer activity of 20(%S%)-camptothecin, a novel class of 20(%S%)-20-%O%-camptothecin %β%-aminopropionates were designed and synthesized with camptothecins as the starting materials, through acylation with acryloyl chloride followed by Michael′s addition. Twelve esters, 1a—1d, 4a—4d and 5a—5d, were synthesized and evaluated by using MTT assay method. The results demonstrate that all these compounds show a potential cytotoxicity on KB, HT-29, HCT-8, and Bel7402 tumor cell lines. Some compounds, 1d, 4c, 5b, 5c and 5d, show a higher cytoto-{xicity} on KB and HCT-8 compared with camptothecin.
To improve the biological anticancer activity of 20 (% S%) -camptothecin, a novel class of 20 (% S%) - 20-% O% -camptothecin% β% -aminopropionates were designed and synthesized with camptothecins as the starting materials, through acylation with acryloyl chloride followed by Michael’s addition. Twelve esters, 1a-1d, 4a-4d and 5a-5d, were synthesized and evaluated by using the MTT assay method. The results demonstrate that all these compounds show a potential cytotoxicity on KB , HT-29, HCT-8, and Bel7402 tumor cell lines. Some compounds, 1d, 4c, 5b, 5c and 5d, show a higher cytoto- {xicity} on KB and HCT-8 than with camptothecin.