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Experimental antitumor activity of taxotere (RP 56976, NSC 628503), a taxol analogue.
TLDR
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.
TLDR
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
TLDR
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.
TLDR
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).
TLDR
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.
TLDR
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.
Intoplicine (RP 60475) and its derivatives, a new class of antitumor agents inhibiting both topoisomerase I and II activities.
TLDR
Study of the relationships between the in vivo antitumor activity on P388 leukemia and the topoisomerase I- and/or II-mediated DNA cleavage activity revealed that the most highly active antitumors compounds possessed both topoisomersase I and II-and II-inhibitory properties.
Purification and characterization of human DNA topoisomerase IIIα
TLDR
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.
TLDR
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.
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