2. Academic Validation
  3. Biological evaluation of some new N-(2,6-dimethoxypyrimidinyl) thioureido benzenesulfonamide derivatives as potential antimicrobial and anticancer agents

Biological evaluation of some new N-(2,6-dimethoxypyrimidinyl) thioureido benzenesulfonamide derivatives as potential antimicrobial and anticancer agents

  • Eur J Med Chem. 2016 Nov 29:124:299-310. doi: 10.1016/j.ejmech.2016.08.060.
Mostafa M Ghorab 1,  Mansour S Alsaid 2,  Mohamed S A El-Gaby 3,  Nesreen A Safwat 4,  Mahmoud M Elaasser 4,  Aiten M Soliman 5
Affiliations

Affiliations

  • 1 Department of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh, 11451, Saudi Arabia; Department of Drug Radiation Research, National Center for Radiation Research and Technology, Atomic Energy Authority, Cairo, Egypt. Electronic address: mmsghorab@yahoo.com.
  • 2 Department of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh, 11451, Saudi Arabia.
  • 3 Department of Chemistry, Faculty of Science, Al-Azhar University in Assiut, Egypt. Electronic address: m_elgaby@hotmail.com.
  • 4 The Regional Center for Mycology and Biotechnology, Al-Azhar University, Cairo, Egypt.
  • 5 Department of Drug Radiation Research, National Center for Radiation Research and Technology, Atomic Energy Authority, Cairo, Egypt.
PMID: 27597407 DOI: 10.1016/j.ejmech.2016.08.060
Abstract

A series of novel heterocyclic thioureas 3a-u containing sulfonamide moiety have been synthesized by the condensation of isothiocyanatobenzenesulfonamide 2 with a variety of heterocyclic amines. The newly synthesized heterocyclic thioureas were investigated for their antimicrobial and Anticancer activity. The in vitro Antibacterial and Antifungal activity were done using well diffusion method. Interestingly, compounds 3j and 3m, showed similar or better activity compared with the reference drug against the tested Microorganisms. Although, 3j was less active among its analogues to inhibit the breast carcinoma cells, it exhibit strong broad spectrum antimicrobial activities. However, The results of the cytotoxic activity revealed that compound 3p was the most active against the breast carcinoma cell line (MCF-7) giving promising IC50 value of 1.72 μg/mL, compared with reference drug (5-flourouracil) with IC50 value of 4.8 μg/mL. The most potent compounds in cytotoxic activity 3b and 3p were further docked inside the active site of CAIX and were found to exhibit a proper binding with the active site Amino acids according to their bond lengths, angles and conformational energy.

Keywords

Anticancer; Antimicrobial; Isothiocyanate; Sulfonamide; Thiourea.

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