177611-75-5

Upstream product

• 55857-35-7 (E)-N-(2-aminobenzylidene)-4-methylaniline 
• 177612-00-9 4-Hydroxy-4-(2-hydroxy-ethyl)-1,4,7,8-tetrahydro-pyrano[3,4-f]indolizine-3,6,10-trione 
• 58610-65-4 ethyl 2-(6′-cyan-5′-oxo-3′,5′-dihydro-2′H-spiro[[1,3]dioxolane-2,1′-indolizine]-7′-yl)acetate 
• 177611-70-0 C₂₄H₃₄N₂O₈ 
• 177611-71-1 C₂₄H₃₃NO₉ 
• 177611-69-7 C₂₂H₂₈N₂O₇ 
• 177611-72-2 C₂₀H₂₅NO₇ 
• 177611-73-3 C₁₅H₁₇NO₇ 
• 73427-84-6 4-Hydroxy-4-(2-methoxy-ethyl)-1,12-dihydro-4H-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione 

Relevant academic research and scientific papers

Synthesis and in vitro cytotoxicity of (RS)-20-desethyl-20-substituted camptothecin analogues

Sixteen (RS)-20-desethyl-20-substituted camptothecin analogues were designed and prepared by total synthesis. These analogues were evaluated for cytotoxic activity against five tumor cell lines. The cytotoxic activity of compound 14f was shown to be comparable to that of camptothecin.

Plant Antitumor Agents. 30. Synthesis and Structure Activity of Novel Camptothecin Analogs

A large number of camptothecin (CPT) analogs have been prepared in the 20S, 20RS, and 20R configurations with a number of ring A substituents.Topoisomerase I (T-I) inhibition data (IC50) have been obtained by standard procedures.In general, substitution at the 9 or 10 positions with amino, halogeno, or hydroxyl groups in compounds with 20S configuration results in compounds with enhanced T-1 inhibition.Compounds in the 20RS configuration were less active in vitro and in vivo and those in the 20R configuration were inactive.Compounds with 10,11-methylenedioxy substitution on ring A displayed a marked increase in potency in the T-I inhibition assay.The activities of some of the analogs as determined in a variety of in vivo assays including the L-1210 mouse leukemia assay were, in general, in accord with T-I inhibition.A number of water-soluble analogs such as 20-glycinate esters, 9-glycinamides, or hydrolyzed lactone salts were prepared and tested in in vitro and in vivo assays.In general, these compounds were less active than CPT both in terms of T-I inhibition and life prolongation in the L-1210 assay.However, certain 20-glycinate esters showed good in vivo activity after iv administration.