Research Topics
| Klaus MullerSummaryCountry: Germany Publications
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Publications
Current status and recent developments in anthracenone antipsoriaticsK Muller
Institut fur Pharmazeutische Chemie, Westfalische Wilhelms Universitat Munster, Hittorfstrasse 58 62, Munster, D 48149, Germany
Curr Pharm Des 6:901-18. 2000..In particular, derivatives bearing a phenylacyl substituent in the critical 10-position of the anthracenone molecule have a favorable overall profile for achieving improved topical therapy of psoriasis...
Ilex aquifolium: protection against enzymatic and non-enzymatic lipid peroxidationK Muller
Institut fur Pharmazeutische Chemie, Westfalische Wilhelms Universitat Munster, Germany
Planta Med 64:536-40. 1998..aquifolium against non-enzymatic lipid peroxidation and deoxyribose degradation...
2-Arylalkyl-substituted anthracenones as inhibitors of 12-lipoxygenase enzymes. 2. Structure-activity relationships of the linker chainKlaus Muller
Westfalische Wilhelms Universitat Munster, Institut fur Pharmazeutische und Medizinische Chemie, Hittorfstrasse 58 62, D 48149 Munster, Germany
Eur J Med Chem 37:83-9. 2002..However, none of the linker chains of the 2-substituted anthracenones provided inhibitors that were able to discriminate between the 12-LO isoforms...
2-arylalkyl-substituted anthracenones as inhibitors of 12-lipoxygenase enzymes. 1. Structure-activity relationships of the terminal aryl ringK Muller
Westfalische Wilhelms Universitat Munster, Institut fur Pharmazeutische Chemie, Hittorfstrasse 58 62, D 48149, Munster, Germany
Eur J Med Chem 36:569-75. 2001..Among the more lipophilic inhibitors, the unsubstituted 2-phenylmethyl analogue 6a as well as the carboxylic acid ester 6q appeared to be selective inhibitors of platelet-type 12-LO isoform...
Pharmaceutically relevant metabolites from lichensK Muller
Institut fur Pharmazeutische Chemie, Westfalische Wilhelms Universitat Munster, Germany
Appl Microbiol Biotechnol 56:9-16. 2001..An improved access to these lichen substances in drug discovery high-throughput screening programs will provide impetus for identifying novel lead-compounds with therapeutic potential and poses new challenges for medicinal chemistry...
10-Phenylbutyryl-substituted anthracenones as inhibitors of keratinocyte growth and LTB(4) biosynthesisK Muller
Westfalische Wilhelms Universitat Munster, Institut fur Pharmazeutische Chemie, Hittorfstrasse 58 62, D 48149, Munster, Germany
Eur J Med Chem 36:179-84. 2001..In contrast to anthralin, cytotoxic effects against cell membranes are strongly reduced as documented by the LDH activity released from cytoplasm of keratinocytes...
Antipsoriatic anthrones with modulated redox properties. 5. Potent inhibition of human keratinocyte growth, induction of keratinocyte differentiation, and reduced membrane damage by novel 10-arylacetyl-1,8-dihydroxy-9(10H)-anthracenonesK Muller
Institut fur Pharmazeutische Chemie, Westfalische Wilhelms Universitat Munster, Hittorfstrasse 58 62, D 48149 Munster, Germany
J Med Chem 44:814-21. 2001..This newly uncovered activity of the novel anthracenones suggests antipsoriatic potential with respect to disturbance of keratinocyte differentiation, in addition to hyperproliferative and inflammatory aspects of psoriasis...
Heterocyclic substituted anthralin derivatives as inhibitors of keratinocyte growth and inducers of differentiationK Muller
Institut fur Pharmazeutische Chemie, Westfalische Wilhelms Universitat Munster, Germany
Bioorg Med Chem Lett 11:47-50. 2001..As a benefit of its strongly diminished potential to generate oxygen radicals, 2e did not induce damage of keratinocyte membranes...
Potential antipsoriatic agents: lapacho compounds as potent inhibitors of HaCaT cell growthK Muller
Institut fur Pharmazeutische Chemie, Westfalische Wilhelms Universitat Munster, Hittorfstrasse 58 62, D 48149 Munster, Germany
J Nat Prod 62:1134-6. 1999..Because of their potent activity against the growth of human keratinocytes, some lapacho-derived compounds appear to be promising as effective antipsoriatic agents...
10-omega-phenylalkyl-9(10H)-anthracenones as inhibitors of keratinocyte growth with reduced membrane damaging propertiesK Muller
Institut fur Pharmazeutische Chemie, Westfalische Wilhelms Universitat Munster, Germany
Bioorg Med Chem Lett 8:3211-6. 1998..In contrast to anthralin, induction of membrane injury is strongly reduced as documented by the release of LDH activity from cytoplasm of keratinocytes...
Phenylimino-10H-anthracen-9-ones as novel antimicrotubule agents-synthesis, antiproliferative activity and inhibition of tubulin polymerizationHelge Prinz
Institute of Pharmaceutical and Medicinal Chemistry, Westphalian Wilhelms University, Hittorfstrasse 58 62, D 48149 Munster, Germany
Bioorg Med Chem 19:4183-91. 2011..The results obtained demonstrate that the antiproliferative activity is related to the inhibition of tubulin polymerization...
10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerizationHelge Prinz
Institute of Pharmaceutical and Medicinal Chemistry, Westphalian Wilhelms University, Munster, Germany
J Med Chem 52:1284-94. 2009..In competition experiments, 17b strongly displaced [(3)H]-colchicine from its binding site in the tubulin. The results obtained demonstrate that the antiproliferative activity is related to the inhibition of tubulin polymerization...
Structure-activity relationship studies of acridones as potential antipsoriatic agents. 1. Synthesis and antiproliferative activity of simple N-unsubstituted 10H-acridin-9-ones against human keratinocyte growthAleksandar Putic
Institute of Pharmaceutical and Medicinal Chemistry, Westphalian Wilhelms University of Munster, Hittorfstrasse 58 62, D 48149 Munster, Germany
Eur J Med Chem 45:3299-310. 2010..Also in contrast to anthralin, membrane-damaging effects as documented by the release of lactate dehydrogenase into the culture medium were not observed for acridones...
Synthesis, antiproliferative activity and inhibition of tubulin polymerization by anthracenone-based oxime derivativesGeorg Surkau
Institute of Pharmaceutical and Medicinal Chemistry, Westphalian Wilhelms University, Hittorfstrasse 58 62, D 48149 Munster, Germany
Eur J Med Chem 45:3354-64. 2010..In this context, anthracenone-based oxime ethers and -esters are considered to contribute to the development of novel antiproliferative drugs, based on tubulin interaction...
N-benzoylated phenoxazines and phenothiazines: synthesis, antiproliferative activity, and inhibition of tubulin polymerizationHelge Prinz
Institute of Pharmaceutical and Medicinal Chemistry, Westphalian Wilhelms University, Hittorfstrasse 58 62, D 48149 Münster, Germany
J Med Chem 54:4247-63. 2011..A series of analogues highlight not only the phenoxazine but also the phenothiazine structural scaffold as valuable pharmacophores for potent tubulin polymerization inhibitors, worthy of further investigation...
Synthesis and structure-activity relationships of lapacho analogues. 1. Suppression of human keratinocyte hyperproliferation by 2-substituted naphtho[2,3-b]furan-4,9-diones, activation by enzymatic one- and two-electron reduction, and intracellular generaAlexandra Reichstein
Institute of Pharmaceutical and Medicinal Chemistry, Westphalian Wilhelms University, Hittorfstraße 58 62, D 48149 Munster, Germany
J Med Chem 55:7273-84. 2012..Selected compounds were studied in detail for their capability to generate superoxide radicals both in isolated enzymatic one- and two-electron reduction assays as well as in a HaCaT cell-based assay...
Synthesis, antiproliferative activity and inhibition of tubulin polymerization by 1,5- and 1,8-disubstituted 10H-anthracen-9-ones bearing a 10-benzylidene or 10-(2-oxo-2-phenylethylidene) moietyHolger C Nickel
Institute of Pharmaceutical and Medicinal Chemistry, Westphalian Wilhelms University, Hittorfstrasse 58 62, D 48149 Munster, Germany
Eur J Med Chem 45:3420-38. 2010..In conclusion, the present study improves understanding of the action of anthracenone-based tubulin polymerization inhibitors and contributes to the design of further potent anti-tubulin drugs...
Structure-activity relationship studies of acridones as potential antipsoriatic agents. 2. Synthesis and antiproliferative activity of 10-substituted hydroxy-10H-acridin-9-ones against human keratinocyte growthAleksandar Putic
Institute of Pharmaceutical and Medicinal Chemistry, Westphalian Wilhelms University, Hittorfstraße 58 62, D 48149 Munster, Germany
Eur J Med Chem 45:5345-52. 2010..The most potent inhibitor of keratinocyte hyperproliferation was compound 8a having an N-methyl group and a 1,3-dihydroxy arrangement at the acridone scaffold, with an IC(50) value comparable to that of anthralin...
Synthesis and biological evaluation of novel 10-benzyl-substituted 4,5-dichloro-10H-anthracen-9-ones as inhibitors of keratinocyte hyperproliferationUlrich Kratz
Institute of Pharmaceutical and Medicinal Chemistry, Westphalian Wilhelms University, Hittorfstraße 58 62, D 48149 Munster, Germany
Eur J Med Chem 45:5278-85. 2010..These findings may be rationalized as a benefit of the ineffectiveness of the novel anthrones to interact with the free radical 2,2-diphenyl-1-picrylhydrazyl...
Synthesis of 2,6-aceanthrylenedione, a cyclic vinylog of anthraquinoneHelge Prinz
Institute of Pharmaceutical and Medicinal Chemistry, Westphalian Wilhelms University, Hittorfstrasse 58 62, D 48149 Munster, Germany
J Org Chem 75:3867-70. 2010..10-Oxo-10H-anthracen-9-ylidene) acetyl chloride (5) cyclizes intramolecularly at room temperature in the presence of AlCl(3) to give 6. We found that 6 is a cytotoxic compound that inhibits tubulin polymerization...
