Elaborating 5-(4-Chlorophenyl)-1,3,4-Thiadiazole Scaffold with A P-Tolyl Sulfonamide Moiety Enhances Cytotoxic Activity: Design, Synthesis, in Vitro Cytotoxicity Evaluation, Radiolabelling and in Vivo Pharmacokinetic Study

Document Type : Original Article

Authors

• Rana Magdy El-Masry ¹
• Mohamed A Amin ²
• Mohamed Korani ³
• Simone Giovannuzzi ⁴
• tamer mostafa sakr ⁵
• Hanan Hassan Kadry ⁶
• Claudiu T Supuran ⁷
• Sahar Shaarawy ⁸
• Azza Taher Shalaby ⁹

¹ Elwahat Street, 6 october city, Egypt

² Labeled Compounds Department, Hot Labs Center, Egyptian Atomic Energy Authority, PO13759, Cairo, Egypt.

³ Radioisotopes Production Facility (RPF), Egyptian Second Research Reactor (ETRR‑2), Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt

⁴ Department of NEUROFARBA, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Polo Scientifico, Via U. Schiff 6, 50019, Sesto Fiorentino, Firenze, Italy

⁵ Radioactive Isotopes and Generator Department, Hot Labs Center, Egyptian Atomic Energy Authority, Cairo 13759, Egypt.

⁶ Department of pharmaceutical organic chemistry, Faculty of pharmacy, Cairo University, Cairo, Egypt

⁷ Università degli Studi di Firenze, NEUROFARBA Dept., Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy

⁸ Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo, Egypt

⁹ Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Cairo University, Cairo, Egypt

Abstract

Keywords

• 1
• 3
• 4-thiadiazoles
• sulfonamides
• carbonic anhydrase inhibitors
• anticancer activity
• radioactive tracing study

Main Subjects

• Organic chemistry