构建了六氢喹啉（HHQ）骨架，并用于新一系列抗癌剂的开发。合成了32个新化合物，其中进行了X射线晶体学确定对映体。13个化合物对NCI 60癌细胞系显示了中等到良好的活性，其中10c的GI%均值高达74%。以厄洛替尼作为参考药物，验证了目标化合物对EGFRWT、EGFRT790M和EGFRL858R的抑制活性，其中化合物10d是最佳抑制剂，IC50分别为0.097、0.280和0.051µM，而厄洛替尼的IC50分别为0.082µM、0.342µM和0.055µM。使用正常人肺细胞(IMR-90)验证了安全性。10c和10d在肺癌、HOP-92和细胞系中扰乱了前G1期和G2/M期细胞周期。通过分子对接研究，了解了三种EGFR活性位点的潜在结合相互作用和亲和力。

Hexahydroquinoline (HHQ) scaffold was constructed and recruited for development of new series of anticancer agents. Thirty-two new compounds were synthesised where x-ray crystallography was performed to confirm enantiomerism. Thirteen compounds showed moderate to good activity against NCI 60 cancer cell lines, with GI % mean up to 74% for 10c. Expending erlotinib as a reference drug, target compounds were verified for their inhibiting activities against EGFRWT, EGFRT790M, and EGFRL858R where compound 10d was the best inhibitor with IC50 = 0.097, 0.280, and 0.051 µM, respectively, compared to erlotinib (IC50 = 0.082 µM, 0.342 µM, and 0.055 µM, respectively). Safety profile was validated using normal human lung (IMR-90) cells. 10c and 10d disrupted cell cycle at pre-G1 and G2/M phases in lung cancer, HOP-92, and cell line. Molecular docking study was achieved to understand the potential binding interactions and affinities in the active sites of three versions of EGFRs.