Add time:07/16/2019         Source:sciencedirect.com

A series of novel heterocyclic 4-substituted pyridine-3-sulfonamides 2–13, 15–20 have been synthesized and investigated as inhibitors of four isoforms of zinc enzyme carbonic anhydrase (CA.EC 4.2.1.1), that is the cytosolic CA I and II, and tumor-associated isozymes CA IX and XII. Against the human isozymes hCA I the new compounds showed KI values in the range 169–5400 nM, toward hCA II in range 58.5–1238 nM, against hCA IX in range 19.5–652 nM and against hCA XII in the range of 16.8–768 nM. Compounds 15–19 representing 4-(1H-pyrazol-1-yl)-3-pyridinesulfonamide derivatives showed good hCA IX inhibitory efficacy with KI = 19.5–48.6 nM comparable or more effective than clinically used sulfonamides: AAZ, MZA, EZA, DCP, IND (KI = 24–50 nM). Anticancer evaluation at a single dose 10 μM, against a panel of 60 human tumor cell lines, was performed at the US National Cancer Institute, on compounds 2, 3, 5–13, 16, 17, 19, 20. Among them 6 bearing 4-(3,4,-dichlorophenyl)piperazine moiety showed broad spectrum of growth inhibition in the range 25–89% over 26 cell lines representing all tumors subpanels.

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