Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry

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Abstract

Synthesis and antiproliferative activity of some novel amides of flufenamic acid and diclofenac

Author(s): Tilal Elsaman, Omar A. A. Aldeeb, Tarek Aboul-Fadl and Abdullah Al-Dhfyan

Coupling of the non-steroidal anti-inflammatory drugs (NSAIDs), flufenamic acid 2 and diclofenac 5 with the appropriate amino acid ester 6, using dicyclohexylcarbdiimide (DCC), afforded amides 7-17, respectively. The structures of the newly synthesized amides 7-17 were confirmed on the basis of their spectral data and X-ray single crystal analysis. All the synthesized compounds have been screened for anti-proliferative activity against A549 lung adenocarcinoma and HT-29 colon cancer cells. Compound 17 showed a good anti-proliferative activity IC50 = 25.82 μM compared with the chemotherapeutic agent 5-fluorouracil IC50= 18 μM. Furthermore, compound 8 was more potent than the reference drug with IC50= 15.4μM and cell cycle blockade activity at G0 and S-phase. Compounds 11, 12, 13 and 17 were more potent than the reference drug dichlorofluorescein diacetate (DCF) IC50= 17.81 μM, while the IC50 for these compound ranges from 6.46-13.99 μM.


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