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  1. Article ; Online: Phenylpyrazalopyrimidines as Tyrosine Kinase Inhibitors: Synthesis, Antiproliferative Activity, and Molecular Simulations.

    Chhikara, Bhupender S / Ashraf, Sajda / Mozaffari, Saghar / St Jeans, Nicole / Mandal, Dindyal / Tiwari, Rakesh Kumar / Ul-Haq, Zaheer / Parang, Keykavous

    Molecules (Basel, Switzerland)

    2020  Volume 25, Issue 9

    Abstract: ... ...

    Abstract N
    MeSH term(s) Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Cell Line, Tumor ; Chemistry Techniques, Synthetic ; Dose-Response Relationship, Drug ; Enzyme Activation/drug effects ; Humans ; Molecular Conformation ; Molecular Docking Simulation ; Molecular Dynamics Simulation ; Molecular Structure ; Protein Kinase Inhibitors/chemical synthesis ; Protein Kinase Inhibitors/chemistry ; Protein Kinase Inhibitors/pharmacology ; Pyrimidines/chemical synthesis ; Pyrimidines/chemistry ; Pyrimidines/pharmacology ; Structure-Activity Relationship ; src-Family Kinases/antagonists & inhibitors ; src-Family Kinases/chemistry
    Chemical Substances Antineoplastic Agents ; Protein Kinase Inhibitors ; Pyrimidines ; src-Family Kinases (EC 2.7.10.2)
    Keywords covid19
    Language English
    Publishing date 2020-05-02
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 1413402-0
    ISSN 1420-3049 ; 1431-5165 ; 1420-3049
    ISSN (online) 1420-3049
    ISSN 1431-5165 ; 1420-3049
    DOI 10.3390/molecules25092135
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  2. Article ; Online: Phenylpyrazalopyrimidines as Tyrosine Kinase Inhibitors

    Bhupender S. Chhikara / Sajda Ashraf / Saghar Mozaffari / Nicole St. Jeans / Dindyal Mandal / Rakesh Kumar Tiwari / Zaheer Ul-Haq / Keykavous Parang

    Molecules, Vol 25, Iss 2135, p

    Synthesis, Antiproliferative Activity, and Molecular Simulations

    2020  Volume 2135

    Abstract: ... aldehydes. The Src kinase enzyme assay revealed modest inhibitory activity (half maximal inhibitory ... inhibitory activity against c-Src (IC 50 = 60.4 µM), Btk (IC 50 = 90.5 µM), and Lck (IC 50 = 110 µM ... while it showed no activity against Abl1, Akt1, Alk, Braf, Cdk2, and PKCa. In combination with target selection ...

    Abstract N 1-(α,β-Alkene)-substituted phenylpyrazolopyrimidine derivatives with acetyl and functionalized phenyl groups at α- and β-positions, respectively, were synthesized by the reaction of 3-phenylpyrazolopyrimidine (PhPP) with bromoacetone, followed by a chalcone reaction with differently substituted aromatic aldehydes. The Src kinase enzyme assay revealed modest inhibitory activity (half maximal inhibitory concentration, IC 50 = 21.7–192.1 µM) by a number of PhPP derivatives. Antiproliferative activity of the compounds was evaluated on human leukemia (CCRF-CEM), human ovarian adenocarcinoma (SK-OV-3), breast carcinoma (MDA-MB-231), and colon adenocarcinoma (HT-29) cells in vitro. 4-Chlorophenyl carbo-enyl substituted 3-phenylpyrazolopyrimidine ( 10 ) inhibited the cell proliferation of HT-29 and SK-OV-3 by 90% and 79%, respectively, at a concentration of 50 µM after 96 h incubation. The compound showed modest inhibitory activity against c-Src (IC 50 = 60.4 µM), Btk (IC 50 = 90.5 µM), and Lck (IC 50 = 110 µM), while it showed no activity against Abl1, Akt1, Alk, Braf, Cdk2, and PKCa. In combination with target selection and kinase profiling assay, extensive theoretical studies were carried out to explore the selectivity behavior of compound 10 . Specific interactions were also explored by examining the changing trends of interactions of tyrosine kinases with the phenylpyrazolopyrimidine derivative. The results showed good agreement with the experimental selectivity pattern among c-Src, Btk, and Lck.
    Keywords protein kinase ; phenylpyrazolopyrimidine ; antiproliferative activity ; enzyme inhibition ; molecular simulation ; Organic chemistry ; QD241-441
    Subject code 540
    Language English
    Publishing date 2020-05-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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