Two series of 2-aminopyridine derivatives 6-17 and tyrphostin AG17 analogs 18-22 bearing 4-methylbenzenesulfonamide moiety were designed and synthesized as anticancer compounds. The synthesized compounds were biologically evaluated for their cytotoxic activity against human breast cancer cell line MCF-7. From 2-aminopyridine and tyrphostin AG17 series, compounds 14, 16 and 20 showed the best activities with IC₅₀ values of 20.4, 18.3 and 26.3 µM, respectively compared to E7070 IC₅₀ 36.3 µM. Further biological evaluation of 14, 16 and 20 against cyclin dependent kinase-2 (CDK2) revealed good inhibitory activity with IC₅₀ of 2.53, 1.79 and 2.92 µM, respectively compared to roscovitine IC₅₀ 0.43 µM. Additionally, capability of γ-radiation to augment the cytotoxic activity of 14, 16 and 20 was studied and showed a dramatic increase in the cell killing effect at lower concentrations after irradiation. Docking was used to investigate the possible binding modes of compounds 14, 16 and 20 inside the active site of CDK2 enzyme.

两个系列的2-氨基吡啶衍生物的6 - 17和酪氨酸磷酸化抑制剂AG17类似物18 - 22轴承-4-甲基苯磺酰胺结构部分，设计并作为抗癌化合物合成。从生物学上评估了合成的化合物对人乳腺癌细胞系MCF-7的细胞毒活性。从2-氨基吡啶和酪氨酸磷酸化抑制剂AG17系列，化合物14，16和20显示出与IC最好活动_50个20.4，18.3和26.3μM，的值分别比E7070 IC ₅₀ 36.3μM。进一步的生物学评估14，16和20对细胞周期蛋白依赖性激酶2（CDK2）揭示了与IC良好的抑制活性₅₀分别相对于IC的roscovitine 2.53，1.79和2.92微米，₅₀ 0.43μM。此外，γ辐射的能力以增加的细胞毒活性14，16和20进行了研究，并表明在照射后较低的浓度在细胞杀伤作用的显着增加。对接被用来研究化合物的可能的结合模式14，16和20 CDK2酶的活性位点内。