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2-(Thienothiazolylimino)-1,3-thiazolidin-4-ones inhibit cell division cycle 25 A phosphatase

Abstract : Cell division cycle dual phosphatases (CDC25) are essential enzymes that regulate cell progression in cell cycle. Three isoforms exist as CDC25A, B and C. Over-expression of each CDC25 enzyme is found in cancers of diverse origins. Thiazolidinone derivatives have been reported to display anti-proliferative activities, bactericidal activities and to reduce inflammation process. New 2-(thienothiazolylimino)-1,3-thiazolidin-4-ones were synthesized and evaluated as inhibitors of CDC25 phosphatase. Among the molecules tested, compound 6 inhibited CDC25A with an IC50 estimated at 6.2 +/- 1.0 mu M. The binding of thiazolidinone derivative 6 onto CDC25A protein was reversible. In cellulo, compound 6 treatment led to MCF7 and MDA-MB-231 cell growth arrest. To our knowledge, it is the first time that such 4-thiazolidinone derivatives are characterized as CDC25 potential inhibitor.
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https://hal.univ-lorraine.fr/hal-01518104
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Submitted on : Thursday, May 4, 2017 - 11:32:29 AM
Last modification on : Saturday, February 27, 2021 - 3:29:46 AM

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Sophie Huber-Villaume, Germain Revelant, Estelle Sibille, Stephanie Philippot, Angelica Morabito, et al.. 2-(Thienothiazolylimino)-1,3-thiazolidin-4-ones inhibit cell division cycle 25 A phosphatase. Bioorganic and Medicinal Chemistry, Elsevier, 2016, 24 (13), pp.2920-2928. ⟨10.1016/j.bmc.2016.04.063⟩. ⟨hal-01518104⟩

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