| 摘要 |
<p>Novel Curcumin analogs were designed, synthesized with 1, 5-diaryl-3-oxo-1,4-pentadienyl pharmacophore and evaluated for their antitumor activities in 5 different cell lines; [ovarian cancer (A2780), renal adenocarcinoma (ACHN), prostate cancer (PC-3), colorectal cancer (Hct-116) and a leukemic monocyte lymphoma (U937-GTB)]. Compounds VII and IV exhibited highly potent cytotoxic activity with IC50 values in 1-2.5 μΜ and 11.4-23.2 μM ranges respectively. Also in silico molecular docking study was carried out using Podophyllotoxin-tubulin complex as template to predict the binding affinity of the target compounds to the receptor. On the other hand, in vitro tubulin polymerization assay was performed to both analogs to test their effect on tubulin and results showed that both analogs IV and VII stabilize microtubules with 79.8 % and 60.6 % respectively causing cancer cell apoptosis with the same mechanism as Paclitaxel which it was compared to during the assay.</p> |
