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Acta Pharmaceutica, Vol. 61 No. 4, 2011.

Original scientific paper

https://doi.org/10.2478/v10007-011-0040-4

Sinteza, in vitro antitumorsko ispitivanje i radiosenzitirajuće vrednovanje novih derivata 4-[3-(supstituiranih)tioureido]-N-(kinoksalin-2-il)benzensulfonamida

MOSTAFA M. GHORAB ; Medicinal, Aromatic and Poisonous Plants Research Center (MAPPRC), College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; Department of Drug Radiation Research, National Center for Radiation Research and Technology, PO Box 29, Nasr City, Cairo,
FATMA A. RAGAB ; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo, Egypt
HELMY I. HEIBA ; Department of Drug Radiation Research, National Center for Radiation Research and Technology, PO Box 29, Nasr City, Cairo, Egypt
MARWA G. EL-GAZZAR ; Department of Drug Radiation Research, National Center for Radiation Research and Technology, PO Box 29, Nasr City, Cairo, Egypt
MOSTAFA G. EL-GAZZAR ; Department of Drug Radiation Research, National Center for Radiation Research and Technology, PO Box 29, Nasr City, Cairo, Egypt

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Abstract

Derivati sulfonamida i kinoksalina imaju raznoliko biološko djelovanje, između ostalog i antitumorsko djelovanje. U radu je opisana sinteza novih derivata tioureido sulfakinoksalina. Svim novim spojevima ispitano je antitumorsko djelovanje in vitro na humanoj staničnoj liniji jetre (HEPG 2). Svi ispitani spojevi pokazuju jači učinak nego referentni lijek doksorubicin. Najjači učinak imali su 4-(3-(4-etilbenzoat)tioureido)-N-(kinoksalin-2-il)benzen-sulfonamid (9) (IC50 = 15,6 µmol L1), N-(piridin-2-il)-4-(3-(4-(N-kinoksalin-2-il-sulfamoil)fenil)tioureido)-benzen-sulfonamid (10) (IC50 = 26,8 µmol L1) i N-(kinoksalin-2-il)-4-(3-(4-(N-tiazol-2-ilsulfamoil)fenil)tioureido)benzen-sulfonamid (11) (IC50 = 24,4 µmol L1), dok je IC50 vrijednost bila 71,8 µmol L1. Najaktivniji spojevi 9, 10 i 11 evaluirani su kao radziosenzitirajuća sredstva nakon izlaganja spojeva γ-zračenju (8 kGy).

Keywords

kinoksalin; sulfonamid; antitumorsko djelovanje; radiosenzitirajući učinak

Hrčak ID:

71386

URI

https://hrcak.srce.hr/71386

Publication date:

31.12.2011.

Article data in other languages: english

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