- Evaluation of alkylating and intercalating properties of mannich bases for cytotoxic activity
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A series of new "hybrid compounds", Mannich base derivatives of planar polycyclic/heterocyclic starting materials, was designed and synthesized. The structures of the compounds were confirmed by spectroscopic methods and elemental analysis. Cytotoxicity of compounds was investigated in three cancer cell lines (PC3, HeLa, and MCF7) and one non-tumoral cell line (293 HEK). We tested the DNA-intercalating capability of the molecules by ethidium bromide (EtBr) fluorescence displacement experiment. Compounds' alkylation potency was investigated via in vitro incubation test using 2-mercaptoethanol, a biomimetic nucleophile. The five of the compounds (7s, 9d, 10b, 11b, 12c) are reported for first time in the literature. Our results suggest that compound 9d has a biological activity close to the reference compound doxorubicin, an intercalating agent in clinical use.
- Istanbullu, Huseyin,Erzurumlu, Yalcin,Kirmizibayrak, Petek Ballar,Erciyas, Ercin
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p. 1096 - 1106
(2015/04/14)
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- Naphthyl ketones: A new class of Janus kinase 3 inhibitors
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Potent inhibition of Janus kinase 3 was found for a series of naphthyl(β-aminoethyl)ketones (e.g. 7, pIC50 = 7.1 ± 0.3). Further studies indicated that these compounds fragment in less than 1 h by retro-Michael reaction in the Jak3 in vitro ELISA assay procedure. The breakdown product of 7,2-naphthylvinyl ketone (22, pIC50 = 6.8 ± 0.3) showed very similar inhibitory activity to 7. Compounds 7 (in neutral buffer) and 22 will be useful pharmacological tools for the investigation of the Janus tyrosine kinase Jak3. (C) 2000 Elsevier Science Ltd. All rights reserved.
- Brown, George R.,Bamford, Andrea M.,Bowyer, Jonathan,James, Daniel S.,Rankine, Neil,Tang, Eric,Torr, Vanessa,Culbert, Eric J.
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p. 575 - 579
(2007/10/03)
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