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 starting 5-(4-chlorophenyl)-1,3,4-thiadiazole-2-amine (2) and the positive control Staurosporine. The anticancer activity of compound 3 is at least partly attributed to the inhibition of the tumor-associated human carbonic anhydrase isoforms IX and XII. The high selectivity of compound 3 for cancer cells over normal cells and for tumor-associated CA isoforms IX and XII over the off-target cytosolic isoform II reflects its safety. Pharmacokinetic study of compound 3 was evaluated in a normal mice model based on a radiopharmaceutical chemistry approach.

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 / El-Masry, Rana; Shaarawy, Sahar; Kadry, Hanan; Shalaby, Azza; Supuran, Claudiu; Giovannuzzi, Simone; sakr, tamer; Amin, Mohamed; Korani, Mohamed. - In: EGYPTIAN JOURNAL OF CHEMISTRY. - ISSN 0449-2285. - ELETTRONICO. - 0:(2022), pp. 0-0. [10.21608/ejchem.2022.162655.6977]

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

Supuran, Claudiu;Giovannuzzi, Simone;
2022

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 starting 5-(4-chlorophenyl)-1,3,4-thiadiazole-2-amine (2) and the positive control Staurosporine. The anticancer activity of compound 3 is at least partly attributed to the inhibition of the tumor-associated human carbonic anhydrase isoforms IX and XII. The high selectivity of compound 3 for cancer cells over normal cells and for tumor-associated CA isoforms IX and XII over the off-target cytosolic isoform II reflects its safety. Pharmacokinetic study of compound 3 was evaluated in a normal mice model based on a radiopharmaceutical chemistry approach.
2022
0
0
0
El-Masry, Rana; Shaarawy, Sahar; Kadry, Hanan; Shalaby, Azza; Supuran, Claudiu; Giovannuzzi, Simone; sakr, tamer; Amin, Mohamed; Korani, Mohamed
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in FLORE sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/1307641
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus ND
  • ???jsp.display-item.citation.isi??? 3
social impact