ChemInform Abstract: Some Transformations of Tertiary N‐Furfurylamides of Aromatic and Heteroaromatic Carboxylic Acids under Acidic Conditions.

Строганова, Т. А.; Vasilin, V. K.; Zelenskaya, Elena A.; Red'kin, Viktor M.; Krapivin, G. D.

doi:10.1002/chin.200905100

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“…The 1 H NMR spectrum of the carboxamide derivative 4 showed two exchangeable NH 2 signals at δ 6.89 and δ 7.25 ppm. It is noteworthy that compound 4 was previously reported as unexpected product during acid catalyzed hydrolysis of N 2, N 2-di(5-methyl-2-furylmethyl)-3-amino-4,6-dimethylthieno[2,3- b ]pyridine-2-carboxamide 31 .…”

Section: Resultsmentioning

confidence: 99%

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Synthesis of new pyridothienopyrimidinone derivatives as Pim-1 inhibitors

Naguib

El‐Nassan

Abdelghany

2017

Journal of Enzyme Inhibition and Medicinal Chemistry

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Four series of pyridothienopyrimidin-4-one derivatives were designed and prepared to improve the pim-1 inhibitory activity of the previously reported thieno[2,3-b]pyridines. Significant improvement in the pim-1 inhibition and cytotoxic activity was achieved using structure rigidification strategy via ring closure. Six compounds (6c, 7a, 7c, 7d, 8b and 9) showed highly potent pim-1 inhibitory activity with IC50 of 4.62, 1.18, 1.38, 1.97, 8.83 and 4.18 μM, respectively. Four other compounds (6b, 6d, 7b and 8a) showed moderate pim-1 inhibition. The most active compounds were tested for their cytotoxic activity on three cell lines [MCF7, HCT116 and PC3]. Compounds 7a [the 2-(2-chlorophenyl)-2,3-dihydro derivative] and 7d [the 2-(2-(trifluoromethyl)-phenyl)-2,3-dihydro derivative] displayed the most potent cytotoxic effect on the three cell lines tested consistent with their highest estimated pim-1 IC50 values.

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Section: Resultsmentioning

confidence: 99%

“…Yield: 88%; mp: 260–261 °C 31 ; IR (cm −1 ): 3464, 3417, 3317, 3267 (two NH 2 ), 2924, 2854 (CH-aliphatic), 1666 (C = O); 1 H NMR (DMSO- d 6 ) δ ppm 2.68 (s, 3H, CH 3 ), 2.86 (s, 3H, CH 3 ), 6.89 (s, 2H, NH 2 , D 2 O exchangeable), 7.25 (s, 2H, NH 2 , D 2 O exchangeable); Anal. Calcd for C 10 H 10 BrN 3 OS: C, 40.01; H, 3.36; N, 14.00.…”

Section: Methodsmentioning

confidence: 99%