Design, synthesis, and antiproliferative activities of novel thiazolyl-pyrazole hybrid derivatives


Kuzu B., Ergüç A., Karakuş F., Arzuk E.

Medicinal Chemistry Research, cilt.32, sa.8, ss.1690-1700, 2023 (SCI-Expanded) identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 32 Sayı: 8
  • Basım Tarihi: 2023
  • Doi Numarası: 10.1007/s00044-023-03090-2
  • Dergi Adı: Medicinal Chemistry Research
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, BIOSIS, CAB Abstracts, Chemical Abstracts Core, Chimica, EMBASE, Veterinary Science Database
  • Sayfa Sayıları: ss.1690-1700
  • Anahtar Kelimeler: ADMET, Antiproliferation, SAR, Thiazolyl-pyrazole
  • Van Yüzüncü Yıl Üniversitesi Adresli: Evet

Özet

In this study, a series of derivatives of thiazolyl-pyrazole hybrid structures were designed to search for new heterocyclic compound-based antitumor agents. The designed target structures were synthesized with easy, practical, and efficient procedures. The antiproliferative effect of the synthesized compounds against cancer cell lines A549, MCF-7, and HepG2 was evaluated regarding inhibition concentration and selectivity index against healthy cell line CCD-34Lu. The results overall showed that the compounds had high antiproliferation against cancer cells compared to the doxorubicin-positive control. In particular, compound 11 A549 (SI: 3.58) and HepG2 (SI: 12.36) had high selectivity in cancer cell lines, while compounds 10h and 10o had high selectivity (SI: 10.74 for both) in MCF-7 cancer cell lines. The calculated theoretical pharmacokinetic properties revealed that they could be suitable drug candidates. In addition, in vitro test results indicate a correlation between the structure-activity relationships of the compounds. The various molecular modifications of thiazolyl-pyrazole hybrid compounds are promising for developing new anticancer drug candidates. Graphical Abstract: [Figure not available: see fulltext.].