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Total Synthesis and Anti-Tubulin Activity of Epi-C3 Analogues of Cryptophycin-24
- Source :
- Journal of Medicinal Chemistry. 47:3697-3699
- Publication Year :
- 2004
- Publisher :
- American Chemical Society (ACS), 2004.
-
Abstract
- Epi-C3-cryptophycin-24, epi-C3-m-chlorobenzyl-cryptophycin-24, and the corresponding styrenes were synthesized and tested in vitro against the MCF-7 and multidrug-resistant MCF-7/ADR breast cancer cell lines and in an in vitro tubulin assembly assay. The results demonstrate that the S configuration at the C3 stereocenter is not required to induce potent cytotoxicity and the m-Cl substituent present on the C10 side chain did not induce any large change in activity.
- Subjects :
- Stereochemistry
Antineoplastic Agents
Peptides, Cyclic
Chemical synthesis
Styrenes
Stereocenter
Structure-Activity Relationship
Biopolymers
Tubulin
Cell Line, Tumor
Depsipeptides
Drug Discovery
Humans
skin and connective tissue diseases
Cytotoxicity
Depsipeptide
chemistry.chemical_classification
biology
Stereoisomerism
Drug Resistance, Multiple
Cyclic peptide
In vitro
chemistry
Biochemistry
Drug Resistance, Neoplasm
Cryptophycin
biology.protein
Molecular Medicine
Drug Screening Assays, Antitumor
Subjects
Details
- ISSN :
- 15204804 and 00222623
- Volume :
- 47
- Database :
- OpenAIRE
- Journal :
- Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....60d2c68f441534cee5064b6568a562e4