Bu kayıt için daha yeni bir sürüm var.

Diğer Açık Erişim

Supplementary Information

Halilibrahim CIFTCI; Masami OTSUKA; Mikako FUJITA; Belgin SEVER


Dublin Core

<?xml version='1.0' encoding='utf-8'?>
<oai_dc:dc xmlns:dc="http://purl.org/dc/elements/1.1/" xmlns:oai_dc="http://www.openarchives.org/OAI/2.0/oai_dc/" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" xsi:schemaLocation="http://www.openarchives.org/OAI/2.0/oai_dc/ http://www.openarchives.org/OAI/2.0/oai_dc.xsd">
  <dc:creator>Halilibrahim CIFTCI</dc:creator>
  <dc:creator>Masami OTSUKA</dc:creator>
  <dc:creator>Mikako FUJITA</dc:creator>
  <dc:creator>Belgin SEVER</dc:creator>
  <dc:date>2024-11-20</dc:date>
  <dc:description>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.  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 (BTT1-10 and BTP1-10) were synthesized and examined for their antiproliferative effects on A549 NSCLC and MCF-7 breast cancer cell lines. According to the results, MTT assay showed that BTT-5 induced strong toxicity in A549 cells with the IC50 value of 9.51±3.35 μM compared to lapatinib (IC50 = 16.44±3.92 μM). BTT-5 also presented a high selectivity profile between Jurkat cell line and PBMCs (healthy) (SI= 65.65). Furthermore, BTT-5 augmented apoptosis significantly in A549 cells (18.40%). BTT-5 displayed significant EGFR inhibition (58.32%) and no significant HER2 inhibition at 10 μM concentration interpreting its selective kinase inhibitory effects. Molecular docking assessment indicated that BTT-5 showed high affinity with a different binding profile than lapatinib in the ATP binding cleft of EGFR. Consequently, BTT-5 can serve as a lead for future anti-NSCLC studies.</dc:description>
  <dc:identifier>https://aperta.ulakbim.gov.trrecord/274087</dc:identifier>
  <dc:identifier>oai:aperta.ulakbim.gov.tr:274087</dc:identifier>
  <dc:rights>info:eu-repo/semantics/openAccess</dc:rights>
  <dc:rights>https://creativecommons.org/licenses/by-nc/4.0/</dc:rights>
  <dc:subject>Naphthalene</dc:subject>
  <dc:subject>Pyrazoline</dc:subject>
  <dc:subject>Thiazole</dc:subject>
  <dc:subject>EGFR</dc:subject>
  <dc:subject>NSCLC</dc:subject>
  <dc:subject>Breast cancer</dc:subject>
  <dc:title>Supplementary Information</dc:title>
  <dc:type>info:eu-repo/semantics/other</dc:type>
  <dc:type>other</dc:type>
</oai_dc:dc>
1,146
145
görüntülenme
indirilme
Tüm sürümler Bu sürüm
Görüntülenme 1,146124
İndirme 14545
Veri hacmi 964.2 MB297.1 MB
Tekil görüntülenme 793100
Tekil indirme 12540

Alıntı yap

Halilibrahim CIFTCI, Masami OTSUKA, Mikako FUJITA ve Belgin SEVER. (2024, 20 Kasım). Supplementary Information. https://aperta.ulakbim.gov.tr/record/274087 adresinden erişildi.

Loading...