The highly lipophilic DNA topoisomerase I inhibitor DB-67 displays elevated lactone levels in human blood and potent anticancer activity

Journal of Controlled Release

Volumn 74, Issue 1-3, 2001, Pages 325-333

  Bom, D ^a   Curran, D P ^b   Zhang, J ^c   Zimmer, S G ^d,e   Bevins, R ^d   Kruszewski, S ^a   Howe, J N ^a   Bingcang, A ^a   Latus, L J ^c   Burke, T G ^a,c,e,f  

^a University of Kentucky   (United States)

^b UNIVERSITY OF PITTSBURGH   (United States)

^c Tigen Pharmaceuticals Inc   (United States)

^d Lexington Veterans Affairs Health Care System   (United States)

^e UNIVERSITY OF KENTUCKY   (United States)

^f UNIVERSITY OF KENTUCKY   (United States)

Author keywords

Camptothecin; Human serum albumin; Liposome; Silatecan; Topoisomerase I

Indexed keywords

7 ETHYL 10 HYDROXYCAMPTOTHECIN; 7 SILYLCAMPTOTHECIN DERIVATIVE; 7 TERT BUTYLDIMETHYLSILYL 10 HYDROXYCAMPTOTHECIN; 9 AMINOCAMPTOTHECIN; ANTINEOPLASTIC AGENT; CAMPTOTHECIN; CAMPTOTHECIN DERIVATIVE; DB 148; DB 158; DB 202; DB 67; DILAUROYLPHOSPHATIDYLCHOLINE; DNA TOPOISOMERASE INHIBITOR; HUMAN SERUM ALBUMIN; IRINOTECAN; LACTONE; LIPOSOME; TOPOTECAN; UNCLASSIFIED DRUG;

ANALYTIC METHOD; ANISOTROPY; ANTINEOPLASTIC ACTIVITY; BLOOD; CANCER CELL CULTURE; CANCER THERAPY; CONCENTRATION RESPONSE; CONFERENCE PAPER; CONTROLLED STUDY; DRUG CYTOTOXICITY; DRUG DETERMINATION; DRUG FORMULATION; DRUG POTENCY; DRUG STABILITY; DRUG STRUCTURE; HUMAN; HUMAN CELL; LIPID BILAYER; LIPOPHILICITY; MEMBRANE BINDING; PHARMACOPHORE; PRIORITY JOURNAL; REVERSED PHASE HIGH PERFORMANCE LIQUID CHROMATOGRAPHY;

ANISOTROPY; ANTINEOPLASTIC AGENTS, PHYTOGENIC; CAMPTOTHECIN; CHEMISTRY, PHYSICAL; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; DNA TOPOISOMERASES, TYPE I; DRUG SCREENING ASSAYS, ANTITUMOR; ENZYME INHIBITORS; HUMANS; LACTONES; LIPID BILAYERS; ORGANOSILICON COMPOUNDS; SPECTROMETRY, FLUORESCENCE; TUMOR CELLS, CULTURED;

EID: 0035816198     PISSN: 01683659     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0168-3659(01)00343-1     Document Type: Conference Paper

References (21)

1. Plant antitumor agents. I. The isolation and structure of camptothecin, a novel alkaloidal leukemia and tumor inhibitor from Camptotheca acuminata
2. Plant antitumor agents. 25. Total synthesis and antileukemic activity of ring A substituted camptothecin analogues. Structure-activity correlations
3. Plant antitumor agents. 28. Resolution of a key tricyclic synthon, 5′(RS)-1,5-dioxo-5′-ethyl-5′-hydroxy-2′H,5′H, 6′H-6′-oxopyrano[3′,4′- f]delta 6,8-tetrahydro-indolizine: Total synthesis and antitumor activity of 20(S)- and 20(R)-camptothecin
4. Metabolism and pharmacokinetics of the camptothecin analogue CPT-11 in the mouse
5. DNA topoisomerase I - Targeted chemotherapy of human colon cancer in xenografts
6. Synthesis of water-soluble (aminoalkyl)camptothecin analogues: Inhibition of topoisomerase I and antitumor activity
7. Phase I and pharmcologic studies of topotecan, a novel topoisomerase I inhibitor without and with G-CSF
8. Evaluation of 9-dimethylaminomethyl-10-hydroxycamptothecin against xenografts derived from adult and childhood solid tumors
9. Pediatric phase I trial and pharmacokinetic study of topotecan administered as a 24-hour continuous infusion
10. The current status of camptothecin analogues as antitumor agents
11. Camptothecin induces protein-linked DNA breaks via mammalian DNA topoisomerase I
12. Resistance of human leukemic and normal lymphocytes to drug-induced DNA cleavage and low levels of DNA topoisomerase II
13. Camptothecin effects on DNA synthesis in murine leukemia cells
14. Action of camptothecin on mammalian cells in culture
15. Structure-activity study of the actions of camptothecin derivatives on mammalian topoisomerase I: Evidence for a specific receptor site and a relation to antitumor activity
16. Lipid bilayer partitioning and stability of camptothecin drugs
17. Preferential binding of the carboxylate form of camptothecin by human serum albumin
18. Differential interactions of camptothecin lactone and carboxylate forms with human blood components
19. Liposomal stabilization of camptothecin's lactone ring
20. The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity
21. Potent topoisomerase I inhibition by novel silatecans eliminates glioma proliferation in vitro and in vivo