Mu.Ta.Lig - COST ACTION CA15135


14 June 2016


General information

Name: Kamil
Surname: Musilek
Cell phone number with international prefix: +420737637058
Country: Czech republic
Affiliation: University of Hradec Kralove
Gender: M
Year of the PhD title: 2007
Personal web page:
Previous COST participation: Yes (CM1103)


List of 10 selected publications within last 5 years

1.       Benek, O.; Soukup, O.; Pasdiorova, M.; Hroch, L.; Sepsova, V.; Jost, P.; Hrabinova, M.; Jun, D.; Kuca, K.; Zala, D.; Ramsay, R.R.; Marco-Contelles, J.*; Musilek, K.* Design, synthesis and in vitro evaluation of indolotacrine analogues as multi-target-directed ligands for the treatment of Alzheimer’s disease. ChemMedChem, in press. DOI: 10.1002/cmdc.201500383.
2.       Nepovimova E, Korabecny J, Dolezal R, Babkova K, Ondrejicek A, Jun D, Sepsova V, Horova A, Hrabinova M, Soukup O, Bukum N, Jost P, Muckova L, Kassa J, Malinak D, Andrs M, Kuca K.* Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity. J Med Chem. 2015 Nov 25;58(22):8985-9003. doi: 10.1021/acs.jmedchem.5b01325.
3.       Nepovimova E, Uliassi E, Korabecny J, Peña-Altamira LE, Samez S, Pesaresi A, Garcia GE, Bartolini M, Andrisano V, Bergamini C, Fato R, Lamba D, Roberti M, Kuca K, Monti B, Bolognesi ML.* Multitarget drug design strategy: quinone-tacrine hybrids designed to block amyloid-β aggregation and to exert anticholinesterase and antioxidant effects. J Med Chem. 2014 Oct 23;57(20):8576-89. doi: 10.1021/jm5010804.
4.       Hamulakova S, Janovec L, Hrabinova M, Spilovska K, Korabecny J, Kristian P, Kuca K*, Imrich J. Synthesis and biological evaluation of novel tacrine derivatives and tacrine-coumarin hybrids as cholinesterase inhibitors. J Med Chem. 2014 Aug 28;57(16):7073-84. doi: 10.1021/jm5008648.
5.       Hroch, L.; Aitken, L.; Benek, O.; Dolezal, M.; Kuca, K.; Gunn-Moore, F.; Musilek, K.* Benzothiazoles; Scaffold of interest for CNS targeted drugs. Current Medicinal Chemistry. 2015, vol. 22, no. 6, p. 730-747. DOI: 10.2174/0929867322666141212120631.
6.       Benek, O.; Aitken, L.; Hroch, L.; Kuca, K.; Gunn-Moore, F.; Musilek, K.* A Direct interaction between mitochondrial proteins and amyloid-β peptide and its significance for the progression and treatment of Alzheimer’s disease. Current Medicinal Chemistry. 2015, vol. 22, no. 9, p. 1056-1085. DOI: 10.2174/0929867322666150114163051.
7.       Korabecny, J.; Dolezal, R.; Cabelova, P.; Horova, A.; Hruba, E.; Ricny, J.; Sedlacek, L.; Nepovimova, E.; Spilovska, K.; Andrs, M.; Musilek, K.; Opletalova, V.; Sepsova, V.; Ripova, D.; Kuca, K.* 7-MEOTA-donepezil like compounds as cholinesterase inhibitors: Synthesis, pharmacological evaluation, molecular modeling and QSAR studies. European Journal of Medicinal Chemistry. 2014, vol. 82, no. 1, p. 426-438. DOI: 10.1016/j.ejmech.2014.05.066
8.       Komloova, M.; Horova, A.; Hrabinova, M.; Jun, D.; Dolezal, M.; Vinsova, J.; Kuca, K.; Musilek, K.* Preparation, in vitro evaluation and molecular modelling of pyridinium-quinolinium/isoquinolinium non-symmetrical bisquaternary cholinesterase inhibitors. Bioorganic & Medicinal Chemistry Letters. 2013, vol. 23, no. 24, p. 6663-6666. DOI: 10.1016/j.bmcl.2013.10.043.
9.       Spilovska, K.; Korabecny, J.; Kral, J.; Horova, A.; Musilek, K.; Soukup, O.; Drtinova, L.; Gazova, Z.; Siposova, K.; Kuca, K.* 7-methoxytacrine-adamantylamine heterodimers as cholinesterase inhibitors in Alzheimer’s disease treatment; synthesis, biological evaluation and molecular modeling studies. Molecules. 2013, vol. 18, no. 2, p. 2397-2418. DOI: 10.3390/molecules18022397.
10.    Holas, O.; Musilek, K.; Pohanka, M.; Kuca, K*. Progress in cholinesterase quantification methods. Expert Opinion on Drug Discovery. 2012, vol. 7, no. 12, p. 1207–1223. DOI: 10.1517/17460441.2012.729037.


Main skills and expertise (up to 5)

1.      Medicinal Chemistry
2.      Organic Chemistry
3.      Pharmacy
4.      Toxicology
5.      Drug Design and Development


Main equipment/facilities available in the participants’ lab (up to 5)

1.      Synthetic lab
2.      Analytical lab
3.      Biochemical lab
4.      Molecular biology lab (in progress)
5.      In vivo testing opportunity with our cooperator


Short personal activity proposal for the COST Action CA15135 (max 1000 characters)

We propose to broaden our scope for identifying new MTDL leads with this COST action. For this purpose, we have developed funnel-like system that involve molecular design, synthesis, analysis, in vitro and in vivo evaluation of novel MTDLs. This system can be used for variable targets or target combination within MTDL strategy. Furthermore, this system might be valuable tool for identification of new MTDL leads for drug research and development.



Work Group preference: score from 1 (preferred) to 4 (not preferred)

Work Group of the CA15135 COST Action Score
WG1: Development of new chemical entities 1
WG2: Selection of biological targets and assessment of biological data 2
WG3: Development of chemical databases 4
WG4: Development of Computational methods for multiple ligand design and discovery 3