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
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 L1), N-(piridin-2-il)-4-(3-(4-(N-kinoksalin-2-il-sulfamoil)fenil)tioureido)-benzen-sulfonamid (10) (IC50 = 26,8 µmol L1) i N-(kinoksalin-2-il)-4-(3-(4-(N-tiazol-2-ilsulfamoil)fenil)tioureido)benzen-sulfonamid (11) (IC50 = 24,4 µmol L1), dok je IC50 vrijednost bila 71,8 µmol L1. 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
Publication date:
31.12.2011.
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