Utility of methyl 2-isothiocyanatobenzoate in the synthesis of some new quinazoline derivatives as potential anticancer and radiosensitizing agents

Mostafa M. Ghorab; Fatma A. Ragab; Helmi I. Heiba; Ahmad A. Bayomi

doi:10.1055/s-0031-1300593

Arzneimittelforschung, Table of Contents

Arzneimittelforschung 2011; 61(12): 719-726
DOI: 10.1055/s-0031-1300593

Antibiotics · Antimycotics · Antiparasitics · Antiviral Drugs · Chemotherapeutics · Cytostatics

Editio Cantor Verlag Aulendorf (Germany)

Utility of methyl 2-isothiocyanatobenzoate in the synthesis of some new quinazoline derivatives as potential anticancer and radiosensitizing agents

Mostafa M. Ghorab

¹Medicinal, Aromatic and Poisonous Plants Research Center, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia

,

Fatma A. Ragab

²Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo, Egypt

,

Helmi I. Heiba

³Department of Drug Radiation Research, National Center for Radiation Research and Technology, Atomic Energy Authority, Cairo, Egypt

,

Ahmad A. Bayomi

³Department of Drug Radiation Research, National Center for Radiation Research and Technology, Atomic Energy Authority, Cairo, Egypt

› Author Affiliations

Abstract

Novel quinazolines 4–11, 15 and triazoloquinazolines 12–14 bearing biologically active sulfonamide moieties were synthesized. All the newly synthesized compounds were evaluated for their in vitro anticancer activity against liver cancer cell line (HEPG2). Some of the screened compounds exhibited interesting cytotoxic activity compared to doxorubicin as a reference drug. The most active compounds 13 and 15 were selected and evaluated for their ability to enhance the cell killing effect of γ-radiation, compound 15 was superior to doxorubicin in radiation combination therapy.

Key words

Anticancer drugs - Quinazolines - Radiosensitizers - Sulfonamides

Full Text

References

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