Literature DB >> 24686014

Analogue-based design, synthesis and biological evaluation of 3-substituted-(methylenehydrazono)indolin-2-ones as anticancer agents.

Haytham E Dweedar1, Hoda Mahrous1, Hany S Ibrahim2, Hatem A Abdel-Aziz3.   

Abstract

The docking studies on CDK2 and GSK-3β inspired us to synthesis a series of indoline-2,3-dione hydrazones 10a-l. Treatment of indoline-2,3-dione derivatives 7a-d with hydrazine gave 3-hydrazonoindolin-2-ones 8a-d which were reacted with the appropriate aldehydes 9a-c to yield 3-substituted-(methylenehydrazono)indolin-2-ones 10a-l. Compounds 10a-l showed a significant anticancer activity against human breast cell line MCF-7. Compounds 10c, f, i exhibited the highest activity almost the same of doxorubicin (IC50 = 6.10 μM) with IC50 = 7.75, 6.75, 6.25 μM, respectively.
Copyright © 2014 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Analogue-based design; Cancer; Human breast cell line MCF-7; Indoline-2,3-dione hydrazones; Molecular docking

Mesh：

Substances：

Year:  2014        PMID： 24686014     DOI： 10.1016/j.ejmech.2014.03.058

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN： 0223-5234            Impact factor:   6.514


  9 in total

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Journal:  ACS Med Chem Lett       Date:  2018-12-18       Impact factor: 4.345

Review 2.  A Mini Review on Isatin, an Anticancer Scaffold with Potential Activities against Neglected Tropical Diseases (NTDs).

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Journal:  Pharmaceuticals (Basel)       Date:  2022-04-27

3.  Synthesis, Biological Evaluation and In Silico Studies of Certain Oxindole-Indole Conjugates as Anticancer CDK Inhibitors.

Authors:  Tarfah Al-Warhi; Ahmed M El Kerdawy; Nada Aljaeed; Omnia E Ismael; Rezk R Ayyad; Wagdy M Eldehna; Hatem A Abdel-Aziz; Ghada H Al-Ansary
Journal:  Molecules       Date:  2020-04-27       Impact factor: 4.411

4.  A New CDK2 Inhibitor with 3-Hydrazonoindolin-2-One Scaffold Endowed with Anti-Breast Cancer Activity: Design, Synthesis, Biological Evaluation, and In Silico Insights.

Authors:  Mohammad M Al-Sanea; Ahmad J Obaidullah; Mohamed E Shaker; Garri Chilingaryan; Mohammed M Alanazi; Nawaf A Alsaif; Hamad M Alkahtani; Sultan A Alsubaie; Mohamed A Abdelgawad
Journal:  Molecules       Date:  2021-01-14       Impact factor: 4.411

5.  Novel oxindole/benzofuran hybrids as potential dual CDK2/GSK-3β inhibitors targeting breast cancer: design, synthesis, biological evaluation, and in silico studies.

Authors:  Wagdy M Eldehna; Sara T Al-Rashood; Tarfah Al-Warhi; Razan O Eskandrani; Amal Alharbi; Ahmed M El Kerdawy
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Authors:  Beata Tylińska; Benita Wiatrak; Żaneta Czyżnikowska; Aneta Cieśla-Niechwiadowicz; Elżbieta Gębarowska; Anna Janicka-Kłos
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7.  Design and synthesis of benzothiazole-based SLC-0111 analogues as new inhibitors for the cancer-associated carbonic anhydrase isoforms IX and XII.

Authors:  Tarfah Al-Warhi; Mostafa M Elbadawi; Alessandro Bonardi; Alessio Nocentini; Ahmed A Al-Karmalawy; Nada Aljaeed; Ohoud J Alotaibi; Hatem A Abdel-Aziz; Claudiu T Supuran; Wagdy M Eldehna
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756

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Authors:  Li-Jun Wang; Shuai-Yu Wang; Bo Jiang; Ning Wu; Xiang-Qian Li; Bao-Cheng Wang; Jiao Luo; Meng Yang; Shui-Hua Jin; Da-Yong Shi
Journal:  Mar Drugs       Date:  2015-02-02       Impact factor: 5.118

9.  A Series of Isatin-Hydrazones with Cytotoxic Activity and CDK2 Kinase Inhibitory Activity: A Potential Type II ATP Competitive Inhibitor.

Authors:  Huda S Al-Salem; Md Arifuzzaman; Hamad M Alkahtani; Ashraf N Abdalla; Iman S Issa; Aljawharah Alqathama; Fatemah S Albalawi; A F M Motiur Rahman
Journal:  Molecules       Date:  2020-09-25       Impact factor: 4.411
  9 in total

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