Synthesis and biological evaluation of novel 1,3,4-thiadiazole derivatives as possible anticancer agents

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ACAR ÇEVİK U., OSMANİYE D., LEVENT S., SAĞLIK B. N., KAYA ÇAVUŞOĞLU B., Karaduma A. B., ...Daha Fazla

ACTA PHARMACEUTICA, cilt.70, sa.4, ss.499-513, 2020 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 70 Sayı: 4
  • Basım Tarihi: 2020
  • Doi Numarası: 10.2478/acph-2020-0034
  • Dergi Adı: ACTA PHARMACEUTICA
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Agricultural & Environmental Science Database, BIOSIS, CAB Abstracts, EMBASE, International Pharmaceutical Abstracts, MEDLINE, Veterinary Science Database, Directory of Open Access Journals
  • Sayfa Sayıları: ss.499-513
  • Anahtar Kelimeler: 1,3,4-thiadiazole, anticancer activity, aromatase inhibitory activity, MTT assay, INHIBITORY-ACTIVITY, AMINOGLUTETHIMIDE, HETEROCYCLES, BINDING
  • Anadolu Üniversitesi Adresli: Evet

Özet

The synthesis of new N-(5-substituted-1,3,4-thiadiazol-2-yl)-2-[5-(substituted amino)-1,3,4-thiadiazol-2-yl)thiolacetamide derivatives and investigation of their anticancer activities were the aims of this work. All the new compounds' structures were elucidated by elemental analyses, IR, H-1 NMR, C-13 NMR and MS spectral data. Anticancer activity studies of the compounds were evaluated against MCF-7 and A549 tumor cell lines. In addition, with the purpose of determining the selectivity of cytotoxic activities, the most active compound was screened against a noncancer NIH3T3 cell line (mouse embryonic fibroblast cells). Among the tested compounds, compound 4y (N-(5-ethyl-1,3,4-thiadiazol-2-yl)-2-((5-(p-tolylamino)-1,3,4-thiadiazol-2-yl)thio)acetamide), showed promising cytotoxic activity against MCF7 cancer cell with an IC50 value of 0.084 +/- 0.020 mmol L-1, and against A549 cancer cell with IC50 value of 0.034 +/- 0.008 mmol L compared with cisplatin. The aromatase inhibitory activity was evaluated for compound 4y on MCF-7 cell line showing promising activity with IC50 of 0.062 +/- 0.004 mmol L-1.