Chemical biology & drug design · 2026
Design, Synthesis, and Investigation of the Biological Activities of New Thiadiazole Derivatives With Anticancer Effects.
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Özkay Yusuf, Bal Enes, Kurban Berkant, Osmaniye Derya, Özkan Begüm Nurpelin Sağlık, Kaplancıklı Zafer Asım
Аннотация
Breast cancer is one of the most significant diseases in today's world. Hormone-dependent breast cancers constitute a significant portion of breast cancers. A series of thiadiazole derivative compounds have been designed to provide a rational alternative to aromatase inhibitors, which are actively used in related cancer treatments. The designed compounds were synthesized in three steps, and their structures were elucidated using 1H-NMR, 13C-NMR, and HRMS spectroscopic methods. The inhibitory potentials of the obtained compounds were investigated using in vitro and in silico methods. In the studies conducted, compound 3c stood out with its scores and values. Compound 3c demonstrated inhibitory activity with an IC50 of 4.896 ± 0.210 μM against the tested cell line and an IC50 of 0.078 ± 0.003 μM against aromatase.