Synthesis and antiproliferative activity of some novel amides of flufenamic acid and diclofenac was written by Elsaman, Tilal;Aldeeb, Omar A. A.;Aboul-Fadl, Tarek;Al-Dhfyan, Abdullah. And the article was included in Pharma Chemica in 2016.Synthetic Route of C14H9Cl2NO This article mentions the following:
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, resp. The structures of the newly synthesized amides 7-17 were confirmed on the basis of their spectral data and X-ray single crystal anal. 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 渭M compared with the chemotherapeutic agent 5-fluorouracil IC50 = 18 渭M. Furthermore, compound 8 was more potent than the reference drug with IC50 = 15.4渭M 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 渭M, while the IC50 for these compound ranges from 6.46-13.99 渭M. In the experiment, the researchers used many compounds, for example, 1-(2,6-Dichlorophenyl)-2-indolinone (cas: 15362-40-0Synthetic Route of C14H9Cl2NO).
1-(2,6-Dichlorophenyl)-2-indolinone (cas: 15362-40-0) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Synthetic Route of C14H9Cl2NO
Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles