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Makale Tam Makale Uluslararası 2022

Design, synthesis and antiproliferative activity evaluation of fluorine-containing chalcone derivatives

Serdar BURMAOĞLU, Derya Anıl, Arzu Gobek, Deryanur Kılıç, Derya Yetkin, Nizami Duran, Oztekin Algul

JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS Cilt 40 · Sayı 8 · ss. 3525–3550 · 01.01.2022
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Özet

A series of new chalcones containing fluoro atom at B ring have been designed, synthesized, and evaluated to be antiproliferative activity against a panel of human tumor cell lines. Some of the analogs (8, 9, 12, 45, 46 and 48) displayed powerful antiproliferative effects to certain human tumor cells, but all of them were devoid of any cytotoxicity towards the normal HEK 293. Acridine orange staining data supported that the cytotoxic and antiproliferative effects of the synthesized analogs on tumor cells are mediated through apoptosis. The compounds 12 and 46 manifested concentration-dependent antiproliferative activity in human hepatocellular carcinoma cell lines using an xCELLigence assay. The structures and antiproliferative activity relationship were further supported by in silico molecular docking study of the compounds against tubulin protein which suggests our compounds interference to cell division.

Anahtar kelimeler

CHALCONE anticancer Synthesis BIOLOGICAL EVALUATION DOCKING MTT ANTIPROLIFERATIVE ACTIVITY PREDICTION flour effect DRUG SOLUBILITY

Atıf için künye

BURMAOĞLU, S., Anıl, D., Gobek, A., Kılıç, D., Yetkin, D., Duran, N., & Algul, O. (2022). Design, synthesis and antiproliferative activity evaluation of fluorine-containing chalcone derivatives. JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS, 40(8), 3525–3550. https://doi.org/10.1080/07391102.2020.1848627

BibTeX
@article{burmaoglu2022-77242,
  author = {BURMAOĞLU, Serdar and Anıl, Derya and Gobek, Arzu and Kılıç, Deryanur and Yetkin, Derya and Duran, Nizami and Algul, Oztekin},
  title = {Design, synthesis and antiproliferative activity evaluation of fluorine-containing chalcone derivatives},
  journal = {JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS},
  year = {2022},
  volume = {40},
  number = {8},
  pages = {3525--3550},
  issn = {0739-1102},
  doi = {10.1080/07391102.2020.1848627},
  url = {https://akademik.atauni.edu.tr/yayinlar/77242-design-synthesis-and-antiproliferative-activity-evaluation-of-fluorine}
}