BMS-247550: A novel epothilone analog with a mode of action similar to paclitaxel but possessing superior antitumor efficacy

Clinical Cancer Research

Volumn 7, Issue 5, 2001, Pages 1429-1437

  Lee, F Y F ^a   Borzilleri, R ^a   Fairchild, C R ^a   Kim, S H ^a   Long, B H ^a   Reventos Suarez, C ^a   Vite, G D ^a   Rose, W C ^a   Kramer, R A ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

EPOTHILONE B; EPOTHILONE DERIVATIVE; IXABEPILONE; PACLITAXEL; UNCLASSIFIED DRUG;

ANTINEOPLASTIC ACTIVITY; ARTICLE; BREAST CARCINOMA; CANCER CELL CULTURE; CANCER RESISTANCE; COLON CARCINOMA; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENCY; HUMAN; HUMAN CELL; MICROTUBULE ASSEMBLY; OVARY CARCINOMA; PANCREAS CARCINOMA; PRIORITY JOURNAL;

ADMINISTRATION, ORAL; ANIMALS; ANTINEOPLASTIC AGENTS; BREAST NEOPLASMS; CELL CYCLE; CELL SURVIVAL; COLONIC NEOPLASMS; DISEASE MODELS, ANIMAL; DRUG RESISTANCE, NEOPLASM; EPOTHILONES; EPOXY COMPOUNDS; FEMALE; HUMANS; INFUSIONS, PARENTERAL; MICE; MICE, INBRED BALB C; MICE, INBRED C57BL; MICE, INBRED DBA; NEOPLASM TRANSPLANTATION; OVARIAN NEOPLASMS; PACLITAXEL; PANCREATIC NEOPLASMS; SARCOMA; THIAZOLES; TUBULIN; TUMOR CELLS, CULTURED; TUMOR STEM CELL ASSAY; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 0034895987     PISSN: 10780432     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (22)

1. Epothilone A and B - Novel 16-membered macrolides and cytotoxic activity: Isolation, crystal structure, and conformation in solution
2. Epothilones, a new class of microtubule-stabilizing agents with a Taxol-like mechanism of action
3. Comparison of novel microtubule polymerizing agents, discodermolide and epothilone A/B, with Taxol
4. Preclinical pharmacology of the epothilone B analog BMS-247550 - An epothilone analog possessing potent activity against paclitaxel-sensitive and -resistant human tumors
5. Synthesis, structure proof, and biological activity of epothilone cyclopropanes
6. A novel application of a Pd(O)-catalyzed nucleophilic substitution reaction to the regio- and stereoselective synthesis of lactam analogues of the epothilone natural products
7. Mechanisms of resistance to etoposide and teniposide in acquired resistant human colon and lung carcinoma cell lines
8. Characterization of a cis-diaminedichloroplatinum(II)-resistant human ovarian cancer cell line and its use in evaluation of platinum analogues
9. Comparison of MTT, XTT, and a novel tetrazolium compound MTS for in vitro proliferation and chemosensitivity assays
10. Preparation of tubulin from brain
11. Biologically active taxol analogues with deleted A-ring side chain substituents and variable C-2′ configuration
12. A generalized Wilcoxon test for comparing arbitrarily singly-censored samples
13. Paclitaxel-resistant human ovarian cancer cells have mutant β-tubulins that exhibit impaired paclitaxel-driven polymerization
14. Plant antitumor agents. VI. The isolation and structure of Taxol, a novel antileukemia and antitumor agent from Taxus brevifolia
15. Structure of a synthetic Taxol precursor: N-tert-butoxycarbonyl-10-deacetyl-N-debenzoyltaxol
16. Eleutherobin, a new cytotoxin that mimics paclitaxel (Taxol) by stabilizing microtubules
17. Eleutherobin, a novel cytotoxic agent that induces tubulin polymerization, is similar to paclitaxel (Taxol)
18. Sarcodictyin A and sarcodictyin B novel diterpenoidic alcohols esterified by (E)-N(1)-methylurocanic acid. Isolation from the Mediterranean stolonifer Sarcodictyon roseum
19. Discodermolide, a cytotoxic marine agent that stabilizes microtubules more potently than Taxol
20. (+)-Discodermolide binds to microtubules in stoichiometric ratio to tubulin dimers, blocks Taxol binding, and results in mitotic arrest
21. A common pharmacophore for epothilone and taxanes: Molecular basis for drug resistance conferred by tubulin mutations in human cancer cells
22. Less is more, regularly. Metronomic dosing of cytotoxic drugs can target tumor angiogenesis in mice