20 Kasım 2024 Diğer Açık Erişim

Halilibrahim CIFTCI; Masami OTSUKA; Mikako FUJITA; Belgin SEVER

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    <subfield code="a">&lt;p&gt;Epidermal growth factor receptor (EGFR) and HER2, pioneer members of the receptor tyrosine kinase subfamily, are frequently mutated and/or overexpressed in several types of human cancers, including non-small cell lung cancer (NSCLC) and breast cancer, which are leading causes of cancer-related deaths worldwide. &amp;nbsp;EGFR and HER2-focused anti-NSCLC and anti-breast cancer studies encouraged us to search for new potential agents. For this purpose, in the current work, naphthalene-linked pyrazoline-thiazole hybrids (&lt;strong&gt;BTT1-10 &lt;/strong&gt;and&lt;strong&gt; BTP1-10) &lt;/strong&gt;were synthesized and examined&lt;strong&gt; &lt;/strong&gt;for their antiproliferative effects on A549 NSCLC and MCF-7 breast cancer cell lines. According to the results, MTT assay showed that &lt;strong&gt;BTT-5&lt;/strong&gt; induced strong toxicity in A549 cells with the IC&lt;sub&gt;50&lt;/sub&gt; value of 9.51&amp;plusmn;3.35 &amp;mu;M compared to lapatinib (IC&lt;sub&gt;50 &lt;/sub&gt;= 16.44&amp;plusmn;3.92 &amp;mu;M). &lt;strong&gt;BTT-5&lt;/strong&gt; also presented a high selectivity profile between Jurkat cell line and PBMCs (healthy) (SI= 65.65). Furthermore, &lt;strong&gt;BTT-5&lt;/strong&gt; augmented apoptosis significantly in A549 cells (18.40%). &lt;strong&gt;BTT-5&lt;/strong&gt; displayed significant EGFR inhibition (58.32%) and no significant HER2 inhibition at 10 &amp;mu;M concentration interpreting its selective kinase inhibitory effects. Molecular docking assessment indicated that &lt;strong&gt;BTT-5&lt;/strong&gt; showed high affinity with a different binding profile than lapatinib in the ATP binding cleft of EGFR. Consequently, &lt;strong&gt;BTT-5&lt;/strong&gt; can serve as a lead for future anti-NSCLC studies.&lt;/p&gt;</subfield>
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    <subfield code="a">Masami OTSUKA</subfield>
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    <subfield code="a">Mikako FUJITA</subfield>
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