1-Toluene-sulfonyl-3-[(3'-hydroxy-5'-substituted)-gamma-butyrolactone]-indoles: synthesis, COX-2 inhibition and anti-cancer activities |
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| Authors: | Singh Palwinder Mittal Anu Bhardwaj Atul Kaur Satwinderjeet Kumar Subodh |
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| Affiliation: | Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India. palwinder_singh_2000@yahoo.com |
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| Abstract: | Indoles carrying a cyclic ester (gamma-butyrolactone) at C-3 position have been synthesized by the allylation of 3-indoleglyoxylate followed by iodocyclisation and the nucleophilic replacement of the iodo-group. Screening of these molecules for COX-2 inhibition and anti-cancer activities has identified compounds 10 and 11 as highly potent and selective for COX-2 as well as showing remarkable anti-cancer activities (better than that of indomethacin). |
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