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

Egyptian Journal of Chemistry

Rana El-Masry, Sahar Shaarawy, Hanan Kadry, Azza Shalaby, Claudiu Supuran, Simone Giovannuzzi, tamer sakr, Mohamed Amin, Mohamed Korani

Citations:

2

Abstract

Novel 1,3,4-thiadiazole derivatives (3-5) were designed, synthesized, and screened for cytotoxic activity. Compound 3 bearing substituted benzenesulfonamide scaffold exhibited remarkable potency against breast cancer (MCF-7), hepatoma (HepG2), colon cancer (HCT116), and lung cancer (A549) cells and lower potency on the normal cells (WI-38), as well as, it possesses higher anticancer activity than ...

Keywords

Moiety

Chemistry

In vivo

Cytotoxicity

In vitro

Sulfonamide

Cytotoxic T cell

Pharmacokinetics

Combinatorial chemistry

Scaffold

Stereochemistry

Pharmacology

Biochemistry

Biomedical engineering

Medicine

Biology

Biotechnology

2022

Article

Institution

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

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

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

2-Y Citation Average

0.712

DOI

https://doi.org/10.21608/ejchem.2022.162655.6977

Language

en

Country

Egypt,

Italy