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SAR studies on hydropentalene derivatives--Important core units of biologically active tetramic acid macrolactams and ptychanolides.
Lutz, Vanessa Mannchen, Fabian Krebs, Michael Park, Natja Krüger, Claudia Raja, Aruna Sasse, Florenz Baro, Angelika Laschat, Sabine
Lutz, Vanessa
Mannchen, Fabian
Krebs, Michael
Park, Natja
Krüger, Claudia
Raja, Aruna
Sasse, Florenz
Baro, Angelika
Laschat, Sabine
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Issue Date
2014-07-01
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original manuscript
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supplementary data
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Abstract
Structurally diverse bicyclo[3.3.0]octanes were prepared and tested for their biological activity. Both the antiproliferative activity and the results of phenotypic characterization varied with the substitution patterns. Two derivatives displayed high inhibitory (IC50 ≤3μM) activity against the L-929 cell line, but differed in their mode of action. A cluster analysis with impedance profiling data showed the two compounds in relationship to microtubule interfering compounds. In PtK2 cells treated with both derivatives a perturbing effect on the microtubular network was observed, whereas the actin cytoskeleton in incubated PtK2 cells was disturbed only by one compound. The effects on tubulin and actin polymerization could be confirmed by in vitro polymerization experiments.
Citation
SAR studies on hydropentalene derivatives--Important core units of biologically active tetramic acid macrolactams and ptychanolides. 2014, 22 (13):3252-61 Bioorg. Med. Chem.
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en
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1464-3391