- Synthesis and antitumor activity evaluation of some thienopyrimidine derivatives
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Some novel thienopyrimidine derivatives were synthesized via the reaction of 5- methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-5-carbohydrazide with different carbonyl compounds such as anhydrides, acid chlorides, carbon disulfide, phenyl isothiocyanate, triethyl orthoformate, diethyl acetylene dicarboxylate, acetylacetone, pyrazole-4-carboxaldehyde, and isatin. Also, the reaction of this carbohydrazide derivative with sodium nitrite in the presence of hydrochloric acid to give the corresponding azide derivative was discussed. The latter azide derivative was reacted with different amines to give the corresponding diheteryl urea derivatives. The antitumor activity evaluation of some representative examples of the synthesized compounds was examined against HePG2 and MCF-7 cell lines. Some of the newly synthesized compounds showed significant activity.
- Abou-Elmagd, Wael S. I.,Abou-Elregal, Mohsen K.,Hemdan, Magdy M.,Mohamed, Amira T. A.,Samir, Sandy S.,Youssef, Ahmed S. A.
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- Novel Thienopyrimidones
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This invention relates to thienopyrimidinones and their use as inhibitors of TRPA1 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of fibrotic diseases, inflammatory and auto-immune diseases and CNS-related diseases.
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Paragraph 0171; 0213-0217
(2021/04/17)
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- Structurally Diverse Mitochondrial Branched Chain Aminotransferase (BCATm) Leads with Varying Binding Modes Identified by Fragment Screening
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Inhibitors of mitochondrial branched chain aminotransferase (BCATm), identified using fragment screening, are described. This was carried out using a combination of STD-NMR, thermal melt (Tm), and biochemical assays to identify compounds that b
- Borthwick, Jennifer A.,Ancellin, Nicolas,Bertrand, Sophie M.,Bingham, Ryan P.,Carter, Paul S.,Chung, Chun-Wa,Churcher, Ian,Dodic, Nerina,Fournier, Charlène,Francis, Peter L.,Hobbs, Andrew,Jamieson, Craig,Pickett, Stephen D.,Smith, Sarah E.,Somers, Donald O'N.,Spitzfaden, Claus,Suckling, Colin J.,Young, Robert J.
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p. 2452 - 2467
(2016/04/10)
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- Design and synthesis of novel protein kinase CK2 inhibitors on the base of 4-aminothieno[2,3-d]pyrimidines
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An extension of our previous research work has resulted in a number of new ATP-competitive CK2 inhibitors that have been identified among 4-aminothieno[2,3-d]pyrimidine derivatives. The most active compounds obtained in the course of the research are 3-(5-p-tolyl-thieno[2,3-d]pyrimidin-4-ylamino)-benzoic acid, 5e (NHTP23, IC50 = 0.01 μM), 3-(5-phenyl-thieno[2,3-d]pyrimidin-4-ylamino)-benzoic acid, 5g (NHTP25, IC50 = 0.065 μM) and 3-(6-methyl-5-phenyl-thieno[2,3-d]pyrimidin-4-ylamino)-benzoic acid, 5n (NHTP33, IC50 = 0.008 μM). Structure-activity relationships of the tested 4-aminothieno[2,3-d]pyrimidine derivatives have been studied and their binding mode with ATP-acceptor site of CK2 has been proposed. A negative effect of intramolecular hydrogen bonding in the compounds' structure is discussed.
- Ostrynska, Olga V.,Balanda, Anatoliy O.,Bdzhola, Volodymyr G.,Golub, Andriy G.,Kotey, Igor M.,Kukharenko, Olexander P.,Gryshchenko, Andrii A.,Briukhovetska, Nadiia V.,Yarmoluk, Sergiy M.
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p. 148 - 160
(2016/04/05)
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- THIENOPYRIMIDINES CONTAINING A SUBSTITUTED ALKYL GROUP FOR PHARMACEUTICAL COMPOSITIONS
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The present invention relates to novel thienopyhmidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
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Page/Page column 53
(2011/09/30)
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- THIENOPYRIMIDINES CONTAINING A SUBSTITUTED ALKYL GROUP FOR PHARMACEUTICAL COMPOSITIONS
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The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
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Page/Page column 20
(2011/09/20)
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- BICYCLIC PYRIMIDINE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS
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Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing thienopyrimidine or oxoquinazoline derivatives are disclosed of the general formula (1) or formula (2) where X is a linker and Y is an aromatic moiety or N(R5)(R6).
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- TRANSFORMATIONS OF 5-METHYL-6-CARBETHOXY-3,4-DIHYDROTHIENOPYRIMIDINE FOR SYNTHESIS OF 4-METHOXY-, 4-ALKYLAMINO-, AND OTHER DERIVATIVES OF THIENOPYRIMIDINE
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4-Chloro derivatives of thienopyrimidine are formed by the action of phosphorus oxychloride on 5-methyl- and 5-methyl-6-carbethoxythienopyrimidin-4-ones.Action of nucleophilic reagents (methanol, sodium methylate, primary and secondary amines) on these chloro derivatives gave 4-methoxy-, 4-alkylamino-, and 4-dialkylamino substituted thienopyrimidines.It was found that 4-methoxy derivatives of thienopyrimidines undergo a thermal rearrangement into 3-methyl-substituted thienopyrimid-4-ones.In the bromination of 5-methyl-4-chloro- and 5-methyl-4-methoxy-substituted thienopyrimidines by N-bromosuccinimide, 5-bromomethyl derivatives of thienopyrimidine are formed, from which, by the action of primary and secondary amines, 5-aminomethyl-substituted thienopyrimidines were obtained.A synthesis of 1,2,3,4-tetrahydro-1,3-diazepinothienopyrimidines was also carried out.
- Grinev, A. N.,Kaplina, N. V.
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p. 767 - 770
(2007/10/02)
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