Hu, Wanning, Hoyer, Jan, Neundorf, Ines ORCID: 0000-0001-6450-3991, Govender, Preshendren, Smith, Gregory S. and Schatzschneider, Ulrich (2015). Synthesis of CpM(CO)(3)-DAB and -PAMAM Dendrimer Conjugates and Preliminary Evaluation of Their Biological Activity. Eur. J. Inorg. Chem. (9). S. 1505 - 1511. WEINHEIM: WILEY-V C H VERLAG GMBH. ISSN 1099-0682

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Abstract

Dendrimers of different generations and core structures [diaminobutane poly(propylenimine) (DAB) G1, G2, G3; poly( amidoamine) (PAMAM) G1] were chosen as carriers for bioactive organometallic half-sandwich complexes of the type CpM(CO)(3) (Cp = cyclopentadienyl, M = Mn or Re) to study the influence of these parameters on their biological activity against cancer cells. Structure-activity relationships were determined by variation of the metal center as well as the type, molecular weight, and number of terminal functional groups of the dendrimer conjugates. All conjugates were characterized by IR and NMR spectroscopy as well as HPLC. Their biological activity was determined on MCF-7 human breast cancer cells by the resazurin assay. Interestingly, the mostactive compounds were the first-generation dendrimer conjugates. The Mn and Re series showed nearly the same activities. Thus, the cytotoxicity of the dendrimer conjugates does not seem to directly correlate with the type or number of terminal functional groups. Rather, it points to a mechanism of action that is different from that previously observed for peptide conjugates with similar CpM(CO)(3) functional groups.

Item Type: Journal Article
Creators:
CreatorsEmailORCIDORCID Put Code
Hu, WanningUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Hoyer, JanUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Neundorf, InesUNSPECIFIEDorcid.org/0000-0001-6450-3991UNSPECIFIED
Govender, PreshendrenUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Smith, Gregory S.UNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Schatzschneider, UlrichUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
URN: urn:nbn:de:hbz:38-405903
DOI: 10.1002/ejic.201403060
Journal or Publication Title: Eur. J. Inorg. Chem.
Number: 9
Page Range: S. 1505 - 1511
Date: 2015
Publisher: WILEY-V C H VERLAG GMBH
Place of Publication: WEINHEIM
ISSN: 1099-0682
Language: English
Faculty: Unspecified
Divisions: Unspecified
Subjects: no entry
Uncontrolled Keywords:
KeywordsLanguage
CELL-PENETRATING PEPTIDE; SOLID-PHASE SYNTHESIS; METAL-COMPLEXES; INTRACELLULAR-DISTRIBUTION; ANTIBACTERIAL ACTIVITIES; BIOMEDICAL APPLICATIONS; STARBURST DENDRIMERS; CYTOTOXICITY; DRUG; DNAMultiple languages
Chemistry, Inorganic & NuclearMultiple languages
URI: http://kups.ub.uni-koeln.de/id/eprint/40590

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