Synthesis and biological evaluation of novel aryloxyacetic acid hydrazide derivatives as anticancer agents

ŞENKARDEŞ S., ERDOĞAN Ö., ÇEVİK Ö., KÜÇÜKGÜZEL Ş. G.

SYNTHETIC COMMUNICATIONS, cilt.51, ss.2634-2643, 2021 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 51
  • Basım Tarihi: 2021
  • Doi Numarası: 10.1080/00397911.2021.1945105
  • Dergi Adı: SYNTHETIC COMMUNICATIONS
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, Chemical Abstracts Core, Chimica, EMBASE
  • Sayfa Sayıları: ss.2634-2643
  • Anahtar Kelimeler: Anticancer activity, caspase-3, cresol, cytotoxicity, hydrazone, synthesis, HYDRAZONES, CANCER, APOPTOSIS
  • Marmara Üniversitesi Adresli: Evet

Özet

In our continuing search for new anticancer agents, herein we report the synthesis of 2-(4-chloro-3-methylphenoxy)-N'-[(aryl)methylidene]acetohydrazides 3a-j and the evaluation of their anticancer activities on cell viability, morphological changes and caspase-3 activity in cancer cell lines including gastric cancer (MKN45), cervical cancer (HeLa) and breast cancer (MDA-MB-231) cells. 2-(4-chloro-3-methylphenoxy)-N'-[(4-phenylthiophen-2-yl)methylidene] acetohydrazide 3g presented the strongest growth inhibition against MKN45 gastric cancer cell lines with the IC50 value of 1.471 +/- 0.23 mu M. Moreover, compounds 3b and 3g showed high potency against the HeLa and MDA-MB-231 cell lines having IC50 in the range of 2.38-9.72 mu M. These compounds are more selective for the tested human cancer cells than for the mouse fibroblast cell line (NIH/3T3). As a result of the studies conducted in order to understand the molecular mechanism, compounds 3b and 3g enhanced expression of the caspase-3 pro-apoptotic proteins levels besides caspase-3 gene.