Experimental antitumor activity of taxotere (RP 56976, NSC 628503), a taxol analogue.
- M. Bissery, D. Guénard, F. Guéritte-Voegelein, F. Lavelle
- Medicine, BiologyCancer Research
- 15 September 1991
Taxotere was evaluated for antitumor activity against a variety of transplantable tumors of mice and effected greater than 80% complete regressions of advanced stage disease with both tumors.
Docetaxel (Taxotere): a review of preclinical and clinical experience. Part I: Preclinical experience.
In vivo, the drug was found to be schedule independent and in vitro, the docetaxel concentrations required to reduce murine and human cell survival by 50% ranged from 4 to 35 ng/ml and the cytotoxic effects were greater on proliferating than on non-proliferating cells.
Preclinical Antitumor Activity of Cabazitaxel, a Semisynthetic Taxane Active in Taxane-Resistant Tumors
Cabazitaxel is as active as docetaxel in docentaxel-sensitive tumor models but is more potent than docetAXel in tumor models with innate or acquired resistance to taxanes and other chemotherapies.
Relationships between the structure of taxol analogues and their antimitotic activity.
- F. Guéritte-Voegelein, D. Guénard, F. Lavelle, M. Le Goff, L. Mangatal, P. Potier
- Chemistry, BiologyJournal of Medicinal Chemistry
- 1 March 1991
This structure-activity relationship study shows that inhibition of microtubule disassembly is quite sensitive to the configuration at C-2' and C-3'.
Preclinical evaluation of docetaxel (Taxotere).
- F. Lavelle, M. Bissery, C. Combeau, J. Riou, P. Vrignaud, S. André
- Biology, MedicineSeminars in Oncology
- 1 April 1995
Docetaxel has significant in vivo antitumor activity in the different models generally used for the preclinical evaluation of drugs and is cytotoxic at clinically relevant concentrations against fresh human tumor biopsy specimens in a soft agar cloning system.
Modulation of DNA topoisomerase I activity by p53.
The results show that topoisomerase I and p53 form molecular complexes in vitro as in vivo, and suggest that the p53-mediated response to DNA damage may, at least in part, involve activation of topoisomersase I.
Preclinical evaluation of TXD258, a new taxoid
Purification and characterization of human DNA topoisomerase IIIalpha.
- H. Goulaouic, T. Roulon, O. Flamand, L. Grondard, F. Lavelle, J. Riou
- Biology, ChemistryNucleic Acids Research
It is shown that hTopo IIIalpha is able to relax negatively supercoiled DNA in a distributive manner, leading to the total disappearance of the initial substrate and the appearance of intermediate topoisomers.
The development of telomerase inhibitors: the G-quartet approach.
- J. Mergny, P. Mailliet, F. Lavelle, J. Riou, A. Laoui, C. Hélène
- BiologyAnti-Cancer Drug Design
- 1 August 1999
This work will present briefly the different strategies that have been proposed to achieve efficient telomerase inhibition, with a special emphasis on G-quartet ligands.
RPR112378 and RPR115781: two representatives of a new family of microtubule assembly inhibitors.
These molecules represent a new class of inhibitors of microtubule assembly with potential therapeutic value and are shown to be a highly cytotoxic compound and that RPR115781 is 10, 000-fold less active as an inhibitor of KB cell growth.