Ghorab Mostafa M, Ragab Fatma A, Heiba Helmi I, Bayomi Ahmad A
Medicinal, Aromatic and Poisonous Plants Research Center, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Arzneimittelforschung. 2011;61(12):719-26. doi: 10.1055/s-0031-1300593.
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 gamma-radiation, compound 15 was superior to doxorubicin in radiation combination therapy.
合成了带有生物活性磺酰胺部分的新型喹唑啉4 - 11、15以及三唑并喹唑啉12 - 14。对所有新合成的化合物进行了针对肝癌细胞系（HEPG2）的体外抗癌活性评估。与作为参考药物的阿霉素相比，一些筛选出的化合物表现出有趣的细胞毒性活性。选择了活性最高的化合物13和15，并评估了它们增强γ射线细胞杀伤作用的能力，在放射联合治疗中，化合物15优于阿霉素。
