About: Synthesis and biological activity of 8-azapurine and pyrazolo[4,3-d]pyrimidine analogues of myoseverin

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About: Synthesis and biological activity of 8-azapurine and pyrazolo[4,3-d]pyrimidine analogues of myoseverin Goto Sponge NotDistinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	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. (en) 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). (cs)
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 (en) Syntéza a biologické aktivity 8-azapurinového a pyrazolo[4,3-d]pyrimidinového analogu myoseverinu (cs)
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 (en) Syntéza a biologické aktivity 8-azapurinového a pyrazolo[4,3-d]pyrimidinového analogu myoseverinu (cs)
skos:notation	RIV/61389030:_____/06:00082517!RIV07-AV0-61389030
http://linked.open.../vavai/riv/strany	1405;1411
http://linked.open...avai/riv/aktivita	P S Z
http://linked.open...avai/riv/aktivity	P(GA301/05/0418), P(GP204/03/D231), S, Z(AV0Z50380511), Z(MSM6198959216)
http://linked.open...iv/cisloPeriodika	-
http://linked.open...vai/riv/dodaniDat	2007
http://linked.open...aciTvurceVysledku	Hlobilková, Alice Havlíček, Libor Kryštof, Vladimír Strnad, Miroslav Moravcová, Daniela Paprskářová, Martina
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Ústav experimentální botaniky AV ČR, v. v. i.
http://linked.open...dnocenehoVysledku	502772
http://linked.open...ai/riv/idVysledku	RIV/61389030:_____/06:00082517
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	Myoseverin; Purine; Tubulin (en)
http://linked.open.../riv/klicoveSlovo	Purine Tubulin Myoseverin
http://linked.open...odStatuVydavatele	FR - Francouzská republika
http://linked.open...ontrolniKodProRIV	[3E7971297279]
http://linked.open...i/riv/nazevZdroje	European Journal of Medicinal Chemistry
http://linked.open...in/vavai/riv/obor	CE
http://linked.open...ichTvurcuVysledku	6 (xsd:int)
http://linked.open...cetTvurcuVysledku	8 (xsd:int)
http://linked.open...vavai/riv/projekt	New generations of cyclin-dependent kinase inhibitors with significant anticancer properties Biological activity of new inhibitors of cyclin-dependent kinases
http://linked.open...UplatneniVysledku	2006
http://linked.open...v/svazekPeriodika	41
http://linked.open...iv/tvurceVysledku	Havlíček, Libor Kryštof, Vladimír Strnad, Miroslav Moravcová, Daniela Hlobilková, Alice Paprskářová, Martina Barbier, P. Peyrot, V.
http://linked.open...n/vavai/riv/zamer	Mechanismy regulace růstu a vývoje rostlin na úrovni buněk, orgánů a celých organismů: fyziologické, genetické a molekulárně biologické základy Modulation of signalling and regulatory pathways in normal and cancer cells
issn	0223-5234
number of pages	7 (xsd:int)

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