Literature DB >> 24631358

Antiproliferative activities of halogenated thieno[3,2-d]pyrimidines.

Kartik W Temburnikar1, Sarah C Zimmermann1, Nathaniel T Kim1, Christina R Ross2, Christopher Gelbmann3, Christine E Salomon3, Gerald M Wilson2, Jan Balzarini4, Katherine L Seley-Radtke5.   

Abstract

The in vitro evaluation of thieno[3,2-d]pyrimidines identified halogenated compounds 1 and 2 with antiproliferative activity against three different cancer cell lines. A structure activity relationship study indicated the necessity of the chlorine at the C4-position for biological activity. The two most active compounds 1 and 2 were found to induce apoptosis in the leukemia L1210 cell line. Additionally, the compounds were screened against a variety of other microbial targets and as a result, selective activity against several fungi was also observed. The synthesis and preliminary biological results are reported herein.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Antifungal; Apoptosis; Cytostatic; Heterocyclic chemistry; Thieno[3,2-d]pyrimidine

Mesh：

Substances：

Year:  2014        PMID： 24631358      PMCID： PMC4565497          DOI： 10.1016/j.bmc.2014.02.033

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  39 in total

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2.  Tyrosine kinase inhibitors. 16. 6,5,6-tricyclic benzothieno[3, 2-d]pyrimidines and pyrimido[5,4-b-] and -[4,5-b]ĭndoles as potent inhibitors of the epidermal growth factor receptor tyrosine kinase.

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Review 3.  Targeting apoptosis pathways in lung cancer.

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4.  Observations on the effect of a folic-acid antagonist on transplantable lymphoid leukemias in mice.

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5.  Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors.

Authors:  Alexis Mollard; Steven L Warner; Lee T Call; Mark L Wade; Jared J Bearss; Anupam Verma; Sunil Sharma; Hariprasad Vankayalapati; David J Bearss
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6.  Addition of lithiated 9-deazapurine derivatives to a carbohydrate cyclic imine: convergent synthesis of the aza-C-nucleoside immucillins.

Authors:  G B Evans; R H Furneaux; T L Hutchison; H S Kezar; P E Morris; V L Schramm; P C Tyler
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7.  GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway.

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8.  Design and SAR of thienopyrimidine and thienopyridine inhibitors of VEGFR-2 kinase activity.

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9.  Design, synthesis, and biological activities of new thieno[3,2-d] pyrimidines as selective type 4 phosphodiesterase inhibitors.

Authors:  M I Crespo; L Pagès; A Vega; V Segarra; M López; T Doménech; M Miralpeix; J Beleta; H Ryder; J M Palacios
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  6 in total

1.  Antiproliferative activities of halogenated pyrrolo[3,2-d]pyrimidines.

Authors:  Kartik W Temburnikar; Christina R Ross; Gerald M Wilson; Jan Balzarini; Brian M Cawrse; Katherine L Seley-Radtke
Journal:  Bioorg Med Chem       Date:  2015-06-16       Impact factor: 3.641

2.  Mitotic arrest of breast cancer MDA-MB-231 cells by a halogenated thieno[3,2-d]pyrimidine.

Authors:  Christina R Ross; Kartik W Temburnikar; Gerald M Wilson; Katherine L Seley-Radtke
Journal:  Bioorg Med Chem Lett       Date:  2015-03-07       Impact factor: 2.823

3.  Anticancer Properties of Halogenated Pyrrolo[3,2-d]pyrimidines with Decreased Toxicity via N5 Substitution.

Authors:  Brian M Cawrse; Rena S Lapidus; Brandon Cooper; Eun Yong Choi; Katherine L Seley-Radtke
Journal:  ChemMedChem       Date:  2017-12-18       Impact factor: 3.466

4.  Design, Synthesis and Anti-Proliferative Activities of 2,6-Substituted Thieno[3,2-d]pyrimidine Derivatives Containing Electrophilic Warheads.

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Journal:  Molecules       Date:  2017-05-12       Impact factor: 4.411

5.  Antitumour, acute toxicity and molecular modeling studies of 4-(pyridin-4-yl)-6-(thiophen-2-yl) pyrimidin-2(1H)-one against Ehrlich ascites carcinoma and sarcoma-180.

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Journal:  Heliyon       Date:  2018-06-27

Review 6.  Thienopyrimidine: A Promising Scaffold to Access Anti-Infective Agents.

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Journal:  Pharmaceuticals (Basel)       Date:  2021-12-27
  6 in total

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