Inhibice polymerace tubulinu myoseverinem a jeho 8-aza analogem

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F04%3A00002414" target="_blank" >RIV/61989592:15310/04:00002414 - isvavai.cz</a>

Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

Inhibition of microtubule assembly by myoseverin and its 8-aza analogue

Popis výsledku v původním jazyce

Microtubules, important structural component of cytoskeleton, represent one of the best described targets of anticancer agents. Antimitotic agents interacting with microtubular cytoskeleton are also frequently used tools of cell biologist. Trisubstitutedpurine myoseverin was previously reported to induce the reversible fission of myotubes into mononucleated fragments, inhibit microtubule polymerization in vitro and interfere with mitotic spindle assembly leading to the mitotic cell cycle arrest. We describe here the comparison of biological activities of myoseverin and its newly synthesized analogue 8-azamyoseverin, that was prepared as a member of our 8-azapurine library. Both compounds inhibited the polymerization of sheep brain purified tubulin ina dose-dependent manner with IC50 values of 7 and 40 microM. On cellular level, the drugs affected the microtubule network and showed antiproliferative effects on a wide range of cancer cell lines independently of their p53 status. Novel

Název v anglickém jazyce

Inhibition of microtubule assembly by myoseverin and its 8-aza analogue

Popis výsledku anglicky

Microtubules, important structural component of cytoskeleton, represent one of the best described targets of anticancer agents. Antimitotic agents interacting with microtubular cytoskeleton are also frequently used tools of cell biologist. Trisubstitutedpurine myoseverin was previously reported to induce the reversible fission of myotubes into mononucleated fragments, inhibit microtubule polymerization in vitro and interfere with mitotic spindle assembly leading to the mitotic cell cycle arrest. We describe here the comparison of biological activities of myoseverin and its newly synthesized analogue 8-azamyoseverin, that was prepared as a member of our 8-azapurine library. Both compounds inhibited the polymerization of sheep brain purified tubulin ina dose-dependent manner with IC50 values of 7 and 40 microM. On cellular level, the drugs affected the microtubule network and showed antiproliferative effects on a wide range of cancer cell lines independently of their p53 status. Novel

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

CE - Biochemie

OECD FORD obor

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Projekt

<a href="/cs/project/GA303%2F02%2F0875" target="_blank" >GA303/02/0875: Vývoj nové generace inhibitorů cyklin-dependentních kinas:vztahy mezi strukturou a aktivitou, molekulární a in vitro mechanismy účinku</a><br>

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2004

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Anticancer Research

ISSN

0250-7005

e-ISSN

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Svazek periodika

24

Číslo periodika v rámci svazku

-

Stát vydavatele periodika

GR - Řecká republika

Počet stran výsledku

305

Strana od-do

3543

Kód UT WoS článku

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EID výsledku v databázi Scopus

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