Expression and characterization of a recombinant psychrophilic<b>γ</b>-carbonic anhydrase (NcoCA) identified in the genome of the Antarctic cyanobacteria belonging to the genus<i>Nostoc</i>

Luca, Viviana De; Prete, Sonia Del; Vullo, Daniela; Carginale, Vincenzo; Fonzo, Pietro Di; Osman, Sameh M.; ALOthman, Zeid A.; Supuran, Claudiu T.; Capasso, Clemente

doi:10.3109/14756366.2015.1069289

Cited by 8 publications

(1 citation statement)

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“…The 1-aryl-3-(2-hydroxyethylthio)-1-propanone investigated here showed rather low tumor-specificity although they induced apoptosis, suggesting that apoptosis-inducing activity itself does not guarantee the antitumor effects. Chemical modifications of the best compound detected here, EU9, are thus necessary to further evaluate such derivatives for their biological activity, as cytotoxic agents or CA inhibitors [40][41][42][43] . …”

Section: Resultsmentioning

confidence: 99%

Synthesis and bioactivity studies of 1-aryl-3-(2-hydroxyethylthio)-1-propanones

Unluer

Gül

Demirtaş

et al. 2016

Journal of Enzyme Inhibition and Medicinal Chemistry

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A series of Mannich bases having piperidine moiety were reacted with 2-mercaptoethanol, leading to 1-aryl-3-piperidine-4-yl-1-propanone hydrochlorides. The cytotoxicity and carbonic anhydrase inhibitory activities of these new compounds were evaluated. Among the compounds, only one derivative, nitro substituent bearing EU9, showed an effective cytotoxicity, although weak tumor specificity against human oral malignant versus nonmalignant cells. The compound induced apoptosis in HSC-2 oral squamous cell carcinoma cells, but not in human gingival fibroblast. Chemical modifications of this lead are thus necessary to further investigate it as a drug candidate and to obtain compounds with a better activity profile.

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Section: Resultsmentioning

confidence: 99%