Cancer is one of the deadliest diseases to humanity. There is significant progress in treating this disease, but developing some drugs that can fight this disease remains a challenge in the field of medical research. Thirteen new 1,2,3-triazole linked tetrahydrocurcumin derivatives were synthesized by click reaction, including a 1,3-dipolar cycloaddition reaction of tetrahydrocurcumin baring mono-alkyne with azides in good yields, and their in vitro anticancer activity against four cancer cell lines, including human cervical carcinoma (HeLa), human lung adenocarcinoma (A549), human hepatoma carcinoma (HepG2), and human colon carcinoma (HCT-116) were investigated using MTT(3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyltetraz-olium bromide) assay. The newly synthesized compounds had their structures identified using NMR HRMS and IR techniques. Some of prepared compounds, including compounds 4g and 4k, showed potent cytotoxic activity against four cancer cell lines compared to the positive control of cisplatin and tetrahydrocurcumin. Compound 4g exhibited anticancer activity with a IC₅₀ value of 1.09 ± 0.17 μM against human colon carcinoma HCT-116 and 45.16 ± 0.92 μM against A549 cell lines compared to the positive controls of tetrahydrocurcumin and cisplatin. Moreover, further biological examination in HCT-116 cells showed that compound 4g can arrest the cell cycle at the G1 phase. A docking study revealed that the potential mechanism by which 4g exerts its anti-colon cancer effect may be through inhabiting the binding of APC–Asef. Compound 4g can be used as a promising lead for further exploration of potential anticancer agents.

Red blood cells (RBCs) are an excellent choice for cell preparation research because of their biocompatibility, high drug loading, and long half-life. In this study, doxorubicin (DOX) was encapsulated with RBCs as the carrier. The biotin-avidin system binding principle was used to modify biotinylated cyclic arginine-glycine-aspartic acid (cRGD) onto RBC surfaces for accurate targeting, high drug loading, and sustained drug release. The RBC drug delivery system (DDS) was characterized, and the concentration of surface sulfur in the energy spectrum was 6.330%. The physical and chemical properties of RBC DDS were as follows: drug content, 0.857 mg/mL; particle size, 3339 nm; potential value, −12.5 mV; and cumulative release rate, 81.35%. There was no significant change in RBC morphology for up to seven days. The results of the targeting and cytotoxicity studies of RBC DDS showed that many RBCs covered the surfaces of U251 cells, and the fluorescence intensity was higher than that of MCF-7 cells. The IC₅₀ value of unmodified drug-loaded RBCs was 2.5 times higher than that of targeted modified drug-loaded RBCs, indicating that the targeting of cancer cells produced satisfactory inhibition. This study confirms that the RBC DDS has the characteristics of accurate targeting, high drug loading, and slow drug release, which increases its likelihood of becoming a clinical cancer treatment in the future.