Medicinal, Aromatic and Poisonous Plants Research Center (MAPPRC), College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Arch Pharm Res. 2012 Jan;35(1):59-68. doi: 10.1007/s12272-012-0106-y. Epub 2012 Feb 2.
A series of novel 4-(4-substituted-thiazol-2-ylamino)-N-(pyridin-2-yl) benzene-sulfonamides were synthesized and screened for their cytotoxic activity against human breast cancer cell line (MCF-7). Compounds 6, 7, 9, 10, 11, and 14 displayed significant activity against MCF-7 when compared to doxorubicin, which was used as a reference drug. The synergistic effect of Gamma radiation for the most active derivatives 7, 9, and 11 was also studied and their IC(50) values markedly decreased to 11.9 μM, 11.7 μM, and 11.6 μM, respectively.
合成了一系列新型的 4-(4-取代噻唑-2-基氨基)-N-(吡啶-2-基)苯磺酰胺，并对其进行了细胞毒性筛选，以评估其对人乳腺癌细胞系 (MCF-7) 的抑制活性。与用作参比药物的阿霉素相比，化合物 6、7、9、10、11 和 14 对 MCF-7 具有显著的抑制活性。还研究了伽马辐射对最具活性的衍生物 7、9 和 11 的协同作用，它们的 IC50 值分别显著降低至 11.9 μM、11.7 μM 和 11.6 μM。
