In this manuscript, design, rational, synthesisand carbonic anhydrases (CAs) inhibitory profile of the quinoline/pyridine linked indole-3-sulfonamide derivatives were reported. The library of 29newly quinoline/pyridine indole-3-sulfonamide derivatives have been generated and examined against the panel of four physiological relevant human CA isoforms, namely, the cytosolic isoforms hCA I and hCA II and the transmembrane tumor associated isoforms hCA IX and hCA XII. Pyridine indole-3-sulfonamide hybrids are selective inhibit transmembrane tumor associated isoforms hCA IX and hCA XII. However, all synthesized quinoline indole-3-sulfonamide hybrids have inhibitory effect on hCA IX isoforms, whereas few have shown inhibitory activity against hCA II and hCA XII as well. However, among all synthesized compound 6q and6p having good inhibitory activity against hCA IX with Ki 1.47 µM and 1.57 µM respectively.These quinoline/pyridine indole-3-sulfonamide conjugatesmay be regarded as potential leads for hCA IXselective inhibitors as anti-cancer agents.

Synthesis of a new series of quinoline/pyridine indole-3-sulfonamide hybrids as selective carbonic anhydrase IX inhibitors / Singh P.; Sridhar Goud N.; Swain B.; Kumar Sahoo S.; Choli A.; Angeli A.; Singh Kushwah B.; Madhavi Yaddanapudi V.; Supuran C.T.; Arifuddin M.. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - ELETTRONICO. - 70:(2022), pp. 128809.128809-128809.128809. [10.1016/j.bmcl.2022.128809]

Synthesis of a new series of quinoline/pyridine indole-3-sulfonamide hybrids as selective carbonic anhydrase IX inhibitors

Angeli A.;Supuran C. T.;
2022

Abstract

In this manuscript, design, rational, synthesisand carbonic anhydrases (CAs) inhibitory profile of the quinoline/pyridine linked indole-3-sulfonamide derivatives were reported. The library of 29newly quinoline/pyridine indole-3-sulfonamide derivatives have been generated and examined against the panel of four physiological relevant human CA isoforms, namely, the cytosolic isoforms hCA I and hCA II and the transmembrane tumor associated isoforms hCA IX and hCA XII. Pyridine indole-3-sulfonamide hybrids are selective inhibit transmembrane tumor associated isoforms hCA IX and hCA XII. However, all synthesized quinoline indole-3-sulfonamide hybrids have inhibitory effect on hCA IX isoforms, whereas few have shown inhibitory activity against hCA II and hCA XII as well. However, among all synthesized compound 6q and6p having good inhibitory activity against hCA IX with Ki 1.47 µM and 1.57 µM respectively.These quinoline/pyridine indole-3-sulfonamide conjugatesmay be regarded as potential leads for hCA IXselective inhibitors as anti-cancer agents.
2022
70
128809
128809
Singh P.; Sridhar Goud N.; Swain B.; Kumar Sahoo S.; Choli A.; Angeli A.; Singh Kushwah B.; Madhavi Yaddanapudi V.; Supuran C.T.; Arifuddin M.
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/1305648
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