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The Synthesis and Biological Evaluation of N-Substituted 1H-Benzimidazol-2-yl-1H-pyrazole-3,5-diamines

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61389030%3A_____%2F16%3A00460144" target="_blank" >RIV/61389030:_____/16:00460144 - isvavai.cz</a>

  • Alternative codes found

    RIV/61989592:15310/16:33160832

  • Result on the web

    <a href="http://dx.doi.org/10.1002/jhet.2315" target="_blank" >http://dx.doi.org/10.1002/jhet.2315</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1002/jhet.2315" target="_blank" >10.1002/jhet.2315</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    The Synthesis and Biological Evaluation of N-Substituted 1H-Benzimidazol-2-yl-1H-pyrazole-3,5-diamines

  • Original language description

    The synthesis of 1H-benzimidazol-2-yl-1H-pyrazole-3,5-diamines has been developed. Synthesized bisheteroaryls contain two privileged medicinal scaffolds, aminopyrazole and benzimidazole, with two diversity positions at N1 of benzimidazole and C3 of pyrazole, respectively. The three-step synthesis includes the Mitsunobu N-alkylation of benzimidazole and subsequent one-pot formation of aminopyrazole involving substitution of methylthio groups with amine and hydrazine followed with final ring closure. Inhibitory activity toward cyclin-dependent kinase 2/cyclin E and cytotoxicity against two cancer cell lines were evaluated for all novel pyrazoles. Two compounds showed modest cyclin-dependent kinase inhibition activity and cytotoxicity against cancer cell lines K562 and MCF7.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

  • CEP classification

    CE - Biochemistry

  • OECD FORD branch

Result continuities

  • Project

    Result was created during the realization of more than one project. More information in the Projects tab.

  • Continuities

    I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Others

  • Publication year

    2016

  • Confidentiality

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

Data specific for result type

  • Name of the periodical

    Journal of Heterocyclic Chemistry

  • ISSN

    0022-152X

  • e-ISSN

  • Volume of the periodical

    53

  • Issue of the periodical within the volume

    2

  • Country of publishing house

    US - UNITED STATES

  • Number of pages

    9

  • Pages from-to

    499-507

  • UT code for WoS article

    000373397600022

  • EID of the result in the Scopus database