Novel Thioether‐Bridged 2,6‐Disubstituted and 2,5,6‐Trisubstituted Imidazothiadiazole Analogues: Synthesis, Antiproliferative Activity, ADME, and Molecular Docking Studies
 
Yazarlar (6)
Öğr. Gör. Ibrahim Ozcan Karabük Üniversitesi, Türkiye
Prof. Dr. Senem Akkoç Süleyman Demirel Üniversitesi, Türkiye
Doç. Dr. Hakan Alıcı Zonguldak Bulent Ecevit University, Türkiye
Dr. Öğr. Üyesi Seval Çapanlar Zonguldak Bulent Ecevit University, Türkiye
Prof. Dr. Onur ŞAHİN Sinop Üniversitesi, Türkiye
Hakan Tahtacı Karabük Üniversitesi, Türkiye
Makale Türü Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
Dergi Adı Chemistry and Biodiversity (Q2)
Dergi ISSN 1612-1872 Dergi Bilgileri (2022)
Dergi Tarandığı Indeksler SCI-Expanded
Makale Dili İngilizce Basım Tarihi 12-2022
Kabul Tarihi 29-11-2022 Yayınlanma Tarihi 13-12-2022
Cilt / Sayı / Sayfa 20 / 1 / – DOI 10.1002/cbdv.202200884
Makale Linki http://dx.doi.org/10.1002/cbdv.202200884
UAK Araştırma Alanları
Yoğun Madde Fiziği
Özet
In this study, starting from 2‐amino‐1,3,4‐thiadiazole derivatives (3–5), a new series of 2,6‐disubstituted (compounds 7–15) and 2,5,6‐trisubstituted (compounds 16–33) imidazo[2,1‐b][1,3,4]‐thiadiazole derivatives were synthesized using cyclization and Mannich reaction mechanisms, respectively. All synthesized compounds were characterized by 1H‐NMR, 13C‐NMR, FT‐IR, elemental analysis, and mass spectroscopy techniques. Also, X‐ray diffraction analysis were used for compounds 4, 7, 11, 17, and 19. The cytotoxic effects of the new compounds on the viability of colon cancer cells (DLD‐1), lung cancer cells (A549), and liver cancer cells (HepG2) were investigated using the 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide (MTT) method in vitro. Compound 15 was found to be the most potent anticancer drug candidate in this series with an IC50 value of 3.63 μM against HepG2 for 48 h …
Anahtar Kelimeler
ADME | antiproliferative activity | bioorganic chemistry | cytotoxicity | heterocycles