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SYNTHESIS AND ANTITUMOR ACTIVITY OF 4-β-ALKOXYLCARBONYL-4-DEOXY-4′-DEMETHYLEPIPODOPHYLLOTOXIN

Chen Zai

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Abstract

AIM To search for more potential and lower toxicity antitumor drugs. METHODS AND RESULTS Thirty eight new 4 β ester substituted 4 deoxy 4′ demethylepipodophylotoxin derivatives(II 1～II 38) were designed and synthesized. All compounds were screened in vitro against L 1210 leukemia and KB cells. CONCLUSION Fatty esters showed higher activity than aromatic esters. II 10 exhibited the highest activity, which is more than 100 fold of etoposide. For fatty esters, the compounds with less than 3 carbons in the main chain have higher activity, while for aromatic esters, those having electron attracting substituents in the aromatic ring are more active.

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AIM To search for more potential and lower toxicity antitumor drugs. METHODS AND RESULTS Thirty eight new 4 β ester substituted 4 deoxy 4′ demethylepipodophylotoxin derivatives(II 1～II 38) were designed and synthesized. All compounds were screened in vitro against L 1210 leukemia and KB cells. CONCLUSION Fatty esters showed higher activity than aromatic esters. II 10 exhibited the highest activity, which is more than 100 fold of etoposide. For fatty esters, the compounds with less than 3 carbons in the main chain have higher activity, while for aromatic esters, those having electron attracting substituents in the aromatic ring are more active.

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Available abstract

AIM To search for more potential and lower toxicity antitumor drugs. METHODS AND RESULTS Thirty eight new 4 β ester substituted 4 deoxy 4′ demethylepipodophylotoxin derivatives(II 1～II 38) were designed and synthesized. All compounds were screened in vitro against L 1210 leukemia and KB cells. CONCLUSION Fatty esters showed higher activity than aromatic esters. II 10 exhibited the highest activity, which is more than 100 fold of etoposide. For fatty esters, the compounds with less than 3 carbons in the main chain have higher activity, while for aromatic esters, those having electron attracting substituents in the aromatic ring are more active.

Key concepts: Chemistry, Etoposide, In vitro, Stereochemistry, Biochemistry, Biology, Chemotherapy, Genetics

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SYNTHESIS AND ANTITUMOR ACTIVITY OF 4-β-ALKOXYLCARBONYL-4-DEOXY-4′-DEMETHYLEPIPODOPHYLLOTOXIN — Research Paper | ScholarLens