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Statements

Subject Item
n2:RIV%2F61389030%3A_____%2F06%3A00082517%21RIV07-AV0-61389030
rdf:type
n9:Vysledek skos:Concept
dcterms:description
Byla porovnána biologická aktivita známého purinového inhibitoru polymerace tubulinu – myoseverinu - a jeho 8-azapurinového a pyrazolo[4,3-d]pyrimidinového analogu v testu inhibice syntézy tubulinu, inhibice CDK1 a pritinádorové aktivitě na lidských nádorových buněčných liniích. Pyrazolo[4,3-d]pyrimidinový isomer myoseverinu má vedle inhibičních účinků na syntézu tubulinu (IC50=16microM) i vlastnosti inhibitoru CDK1 (IC50=4microM). The trisubstituted purine myoseverin has been recently identified as a novel inhibitor of microtubule assembly. To analyze the effects of modifying its heterocyclic skeleton, we prepared 8-azapurine and pyrazolo[4,3-d]pyrimidine analogues of myoseverin and compared their biological activities. Rearrangement of nitrogen atoms in the heterocycle changes the affinity of the compounds to purified tubulin, as demonstrated by the results of polymerization assays, and affects the proliferation of cancer cell lines. Surprisingly, compound E2GG, a pyrazolo[4,3-d]pyrimidine analogue of myoseverin, displayed inhibitory activity towards both tubulin polymerization and the activity of cyclin-dependent kinases 1, 2 and 7. Such a dual specificity-inhibitor offers a starting point for developing a novel class of antiproliferative agents. The trisubstituted purine myoseverin has been recently identified as a novel inhibitor of microtubule assembly. To analyze the effects of modifying its heterocyclic skeleton, we prepared 8-azapurine and pyrazolo[4,3-d]pyrimidine analogues of myoseverin and compared their biological activities. Rearrangement of nitrogen atoms in the heterocycle changes the affinity of the compounds to purified tubulin, as demonstrated by the results of polymerization assays, and affects the proliferation of cancer cell lines. Surprisingly, compound E2GG, a pyrazolo[4,3-d]pyrimidine analogue of myoseverin, displayed inhibitory activity towards both tubulin polymerization and the activity of cyclin-dependent kinases 1, 2 and 7. Such a dual specificity-inhibitor offers a starting point for developing a novel class of antiproliferative agents.
dcterms:title
Synthesis and biological activity of 8-azapurine and pyrazolo[4,3-d]pyrimidine analogues of myoseverin Synthesis and biological activity of 8-azapurine and pyrazolo[4,3-d]pyrimidine analogues of myoseverin Syntéza a biologické aktivity 8-azapurinového a pyrazolo[4,3-d]pyrimidinového analogu myoseverinu
skos:prefLabel
Synthesis and biological activity of 8-azapurine and pyrazolo[4,3-d]pyrimidine analogues of myoseverin Synthesis and biological activity of 8-azapurine and pyrazolo[4,3-d]pyrimidine analogues of myoseverin Syntéza a biologické aktivity 8-azapurinového a pyrazolo[4,3-d]pyrimidinového analogu myoseverinu
skos:notation
RIV/61389030:_____/06:00082517!RIV07-AV0-61389030
n3:strany
1405;1411
n3:aktivita
n6:Z n6:S n6:P
n3:aktivity
P(GA301/05/0418), P(GP204/03/D231), S, Z(AV0Z50380511), Z(MSM6198959216)
n3:cisloPeriodika
-
n3:dodaniDat
n16:2007
n3:domaciTvurceVysledku
n7:4712048 n7:2619725 n7:9130241 n7:1870378 n7:9961216 n7:4744756
n3:druhVysledku
n11:J
n3:duvernostUdaju
n8:S
n3:entitaPredkladatele
n4:predkladatel
n3:idSjednocenehoVysledku
502772
n3:idVysledku
RIV/61389030:_____/06:00082517
n3:jazykVysledku
n18:eng
n3:klicovaSlova
Myoseverin; Purine; Tubulin
n3:klicoveSlovo
n14:Tubulin n14:Myoseverin n14:Purine
n3:kodStatuVydavatele
FR - Francouzská republika
n3:kontrolniKodProRIV
[3E7971297279]
n3:nazevZdroje
European Journal of Medicinal Chemistry
n3:obor
n17:CE
n3:pocetDomacichTvurcuVysledku
6
n3:pocetTvurcuVysledku
8
n3:projekt
n15:GA301%2F05%2F0418 n15:GP204%2F03%2FD231
n3:rokUplatneniVysledku
n16:2006
n3:svazekPeriodika
41
n3:tvurceVysledku
Kryštof, Vladimír Havlíček, Libor Hlobilková, Alice Barbier, P. Peyrot, V. Paprskářová, Martina Strnad, Miroslav Moravcová, Daniela
n3:zamer
n12:AV0Z50380511 n12:MSM6198959216
s:issn
0223-5234
s:numberOfPages
7