Literature DB >> 30248510

Synthesis and in vitro antitumor evaluation of some new thiophenes and thieno[2,3-d]pyrimidine derivatives.

Mahasen M Fouad1, Eman R El-Bendary2, Ghada M Suddek3, Ihsan A Shehata4, Mohamed M El-Kerdawy4.   

Abstract

New thiophene (2-13) and thienopyrimidine (15-27) derivatives have been synthesized. Twenty three compounds were screened against five cell lines namely; hepatocellular carcinoma (liver) HepG-2, epidermoid carcinoma (larynx) Hep-2, mammary gland (breast) MCF-7, human prostate cancer PC-3 and epithelioid cervix carcinoma HeLa. The results revealed that compounds 15,16,17,24 and 25 showed the highest antitumor activity against all tested cell lines compared to Doxorubicin. In order to explain the expected mode of action of the observed anticancer activity, compounds 15,16,17,24 and 25 were selected to screen their DNA binding affinity and enzyme inhibitory activity against DNA polymerase, thymidylate synthase and tyrosine kinase. The results revealed that the tested compounds showed good DNA binding affinity as well as good inhibitory activity against the three enzymes which might explain the observed anticancer activity of the target compounds. Published by Elsevier Inc.

Entities:  

Keywords:  Antitumor evaluation; Synthesis; Thienopyrimidines; Thiophenes

Mesh：

Substances：

Year:  2018        PMID： 30248510     DOI： 10.1016/j.bioorg.2018.09.022

Source DB:  PubMed          Journal:  Bioorg Chem        ISSN： 0045-2068            Impact factor:   5.275


  10 in total

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2.  Biosynthesis of Cu/KF/Clinoptilolite@MWCNTs nanocomposite and its application as a recyclable nanocatalyst for the synthesis of new Schiff base of benzoxazine derivatives and reduction of organic pollutants.

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Review 3.  Recent development in the synthesis of heterocycles by 2-naphthol-based multicomponent reactions.

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4.  Solvent-free synthesis of new spiropyrroloindole compounds using Fe3O4/TiO2/MWCNTs MNCs via multicomponent reactions: assessment of new spiropyrroloindole antioxidant activity.

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Journal:  Mol Divers       Date:  2022-01-31       Impact factor: 3.364

5.  Synthesis of Novel Analogs of Thieno[2,3-d] Pyrimidin-4(3H)-ones as Selective Inhibitors of Cancer Cell Growth.

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Journal:  Biomolecules       Date:  2019-10-21

Review 6.  Nitroketene N,S-acetals: synergistic building blocks for the synthesis of heterocycles.

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Journal:  RSC Adv       Date:  2019-05-09       Impact factor: 4.036

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Journal:  Front Chem       Date:  2022-09-29       Impact factor: 5.545

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Authors:  Tayyebeh Kohestani; S Zahra Sayyed-Alangi; Zinatossadat Hossaini; Mohammad T Baei
Journal:  Mol Divers       Date:  2021-07-24       Impact factor: 2.943

10.  Synthesis and Antibacterial Activities of Different Five-Membered Heterocyclic Rings Incorporated with Pyridothienopyrimidine.

Authors:  Mohamed Ge Zayda; Adel A-H Abdel-Rahman; Farag A El-Essawy
Journal:  ACS Omega       Date:  2020-03-10
  10 in total

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