Abstract
A series of 7-cycloalkylcamptothecin derivatives were synthesized from camptothecin with two methods. Their biological activities in vitro were evaluated with sulforhodamine-B (SRB) method on four types of human tumor cell lines A549/ATCC, HT29, NCI-H460 and HL60. Most of these camptothecin analogues show higher antitumor activity than the reference compounds SN-38 and Topotecan, with the IC(50) values low to nM level. Structure-activity relationship studies of these compounds mostly match the conclusion we achieved before from quantitative structure-activity relationship (QSAR) research.
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / pharmacology
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Camptothecin / administration & dosage*
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Camptothecin / analogs & derivatives
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Camptothecin / chemical synthesis*
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Camptothecin / pharmacology
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Cell Line, Tumor
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Chemistry, Pharmaceutical / methods
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Colorectal Neoplasms / drug therapy
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Drug Design
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Drug Screening Assays, Antitumor
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HL-60 Cells
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Humans
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Hydrolysis
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Inhibitory Concentration 50
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Irinotecan
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Models, Chemical
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Rhodamines / pharmacology
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Structure-Activity Relationship
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Topotecan / chemical synthesis
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Topotecan / pharmacology
Substances
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Antineoplastic Agents
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Rhodamines
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lissamine rhodamine B
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Irinotecan
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Topotecan
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Camptothecin