7-Cycloalkylcamptothecin derivatives: Preparation and biological evaluation.
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.
Li
Mingzong
M
Department of Chemistry, University of Science & Technology of China, Hefei, Anhui 230026, PR China.
Jin
Wei
W
Jiang
Chen
C
Zheng
Chao
C
Tang
Weidong
W
You
Tianpa
T
Lou
Liguang
L
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D002166:Camptothecin / Q000008:administration & dosage* / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015179:Colorectal Neoplasms / Q000188:drug therapy; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D018922:HL-60 Cells; D006801:Humans; D006868:Hydrolysis; D020128:Inhibitory Concentration 50; D000077146:Irinotecan; D008956:Models, Chemical; D012235:Rhodamines / Q000494:pharmacology; D013329:Structure-Activity Relationship; D019772:Topotecan / Q000138:chemical synthesis / Q000494:pharmacology
D000970:Antineoplastic Agents; D012235:Rhodamines; C022027:lissamine rhodamine B; D000077146:Irinotecan; D019772:Topotecan; D002166:Camptothecin