62556-23-4Relevant academic research and scientific papers
Synthesis, characterization and biological evaluation of some new indomethacin analogs with a colon tumor cell growth inhibitory activity
Eissa, Sally I.
, p. 2205 - 2220 (2017)
Focusing particularly on colorectal cancer, and suggesting research strategies that may help to accelerate the future clinical application of indomethacin for the treatment of cancer, the molecular structures of indomethacin was used as starting scaffold to design novel amide analogs, and the effects of those analogs on the proliferation of human cancer cells were evaluated against three colon cancer cell lines, namely, HCT-116, CACO-2, and HT-29. Compared to indomethacin, the new derivatives displayed significantly increased activities. Interestingly two of the indomethacin analogs 7a and 8c displayed high growth inhibitory activity in nano-molar to micro-molar range against all three human colon cancer cell lines with IC50 values ranging from 0.055 to 4.0 μg/ml compared to 0.7–5.45 μg/ml for 5-fluorouracil (5-FU). Moreover, the potential mechanisms of the cytotoxic activity of the promising compounds 7a and 8c on the HT-29 and HCT-116 cell lines respectively were studied. The results indicated that compounds 7a and 8c arrested the cell cycle at G1/S and G0/G1 phase in HT-29 and HCT-116 cells respectively and might induced apoptosis via caspase-3 dependent pathway.
Near-Infrared Fluorescent Heptamethine Cyanine Dyes for COX-2 Targeted Photodynamic Cancer Therapy
Wangngae, Sirilak,Siriwibool, Siriwalee,Chansaenpak, Kantapat,Wet-osot, Sirawit,Lai, Rung-Yi,Kamkaew, Anyanee
supporting information, (2022/02/21)
We designed and synthesized two heptamethine cyanine-based theranostic probes that aimed to target COX-2 in cancer cells. One is I-IR799-CXB, in which I-IR799 is conjugated to the COX-2-specific inhibitor, celecoxib, and another is I-IR799-IMC, where the non-selective COX inhibitor, indomethacin, was used. I-IR799 is a heptamethine cyanine derivative that can be activated by near-infrared light for photodynamic therapy (PDT) purposes. I-IR799-CXB and I-IR799-IMC were tested for their cancer-targeting capacity and photodynamic efficiency toward hepatocellular carcinoma (HepG2) cells relative to normal liver cells, alpha mouse liver 12 (AML12) cells. Interestingly, after conjugation, I-IR799-IMC exhibited better tumour targetability and PDT efficiency than I-IR799-CXB.
