Synthesis and biological evaluation of novel oxadiazole derivatives: A new class of thymidine phosphorylase inhibitors as potential anti-tumor agents

Journal Article

Filipekc, Sohail Anjum Shahzad , Muhammad Yar, Marek Bajda, Bushra Jadoon, Zulfiqar Ali Khane, Syed Ali Raza Naqvie, Ahson Jabbar Shaikha, Khizar Hayata, Adeem Mahmmod, Nasir Mahmood, Sławomir . 2014

• نوع عمل المنشور: Research
• رابط المنشور على الويب: Bioorganic and Medicinal Chemistry
• رقم العدد: 3
• رقم الإصدار السنوي: 22
• الصفحات: 1008-1015

مستخلص المنشور

Based on the fact that the thymidine phosphorylase inhibitors are considered potential anti-tumor agents, a range of novel oxadiazole derivatives 3a–3u was designed and synthesized by a simple and facile synthetic route. The biological assay revealed that majority of compounds displayed modest inhibitory activity against thymidine phosphorylase at low micromolar concentrations (IC50 173.23 ± 3.04 to 14.40 ± 2.45 μM). In the current study the most active compounds were 3h and 3q with IC50 values 14.40 ± 2.45 and 17.60 ± 1.07 μM, respectively. Molecular docking studies were performed on the most active compounds (3h, 3k, 3o–3q) to show their binding mode.