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Synthesis and Biological Evaluation of a Small Molecule Library of 3Rd Generation Multidrug Resistance Modulators by Werner Klinkhammer; Henrik Müller; Christoph Globisch; Ilza K. Pajeva; Michael Wiese is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Synthesis and Biological Evaluation of a Small Molecule Library of 3Rd Generation Multidrug Resistance Modulators about?
The development of new modulators possessing high efficacy, low toxicity and high selectivity is a pivotal approach to overcoming P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in tumour cells. In this study 39 compounds are presented which have been synthesized and pharmacologically investigated in our laboratory. Similarly to the potent 3rd generation MDR modulator tariquidar (XR9576) the compounds contain a tetrahydroisoquinoline-ethyl-phenylamine substructure that, in contrast to XR9576, is connected to a smaller hydrophobic part, thus leading to molecules of lower molecular weight. The connection between the tetrahydroisoquinoline-ethyl-phenylamine substructure and the hydrophobic part was achieved through four different types of linkers: amide, urea, amide-ether and amide-styryl. A number of structural modifications in the hydrophobic part were created. The calcein AM assay served as test system to determine the P-gp transport inhibitory potencies of the compounds. For the amide linker derivatives a structure-activity relationship analysis was performed outlining which structural modifications contributed to the inhibitory potency. The compounds containing a bicycl
Who reads Synthesis and Biological Evaluation of a Small Molecule Library of 3Rd Generation Multidrug Resistance Modulators?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Werner Klinkhammer; Henrik Müller; Christoph Globisch; Ilza K. Pajeva; Michael Wiese
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)
- Published
- 2009
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)