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Literature DB >> 32454626

Synthesis and Pharmacologic Evaluation of Some Benzimidazole Acetohydrazide Derivatives as EGFR Inhibitors.

Serkan Demirel¹, Gülgün Ayhan Kilcigil¹, Zümra Kara², Berna Güven², Arzu Onay Beşikci².

Abstract

OBJECTIVES: In this study, some novel 2-(2-phenyl)-1H-benzo[d]imidazol-1-yl)-N'-(arylmethylene) acetohydrazide derivatives (1-12) were designed and synthesized.
MATERIALS AND METHODS: Compounds 1-12 were obtained by condensing 2-(2-phenyl)-1H-benzo[d]imidazol-1-yl)acetohydrazide (III) with the corresponding aromatic aldehyde derivatives in the presence of catalytic amounts of hydrochloric acid in ethanol.
RESULTS: Following the structure elucidation, epidermal growth factor receptor kinase inhibitor activity was measured. The ADP-GloTM kinase assay determines kinase activity based on the quantification of the amount of ADP produced during a kinase reaction.
CONCLUSION: Almost all of the compounds' kinase inhibitor activities were rather limited. ©Copyright 2017 Turk J Pharm Sci, Published by Galenos Publishing House.

Entities: Chemical

Keywords: Benzimidazole; acetohydrazide; epidermal growth factor receptor kinase; inhibitory

Year: 2017 PMID： 32454626 PMCID： PMC7227932 DOI： 10.4274/tjps.24008

Source DB: PubMed Journal: Turk J Pharm Sci ISSN： 1304-530X

8 in total

Review 1. The protein kinase complement of the human genome.

Authors: G Manning; D B Whyte; R Martinez; T Hunter; S Sudarsanam
Journal: Science Date: 2002-12-06 Impact factor: 47.728

2. Design and synthesis of new (E)-cinnamic N-acylhydrazones as potent antitrypanosomal agents.

Authors: Samir A Carvalho; Larisse O Feitosa; Márcio Soares; Thadeu E M M Costa; Maria G Henriques; Kelly Salomão; Solange L de Castro; Marcel Kaiser; Reto Brun; James L Wardell; Solange M S V Wardell; Gustavo H G Trossini; Adriano D Andricopulo; Edson F da Silva; Carlos A M Fraga
Journal: Eur J Med Chem Date: 2012-06-07 Impact factor: 6.514

3. Discovery of novel benzimidazoles as potent inhibitors of TIE-2 and VEGFR-2 tyrosine kinase receptors.

Authors: Masaichi Hasegawa; Naohiko Nishigaki; Yoshiaki Washio; Kazuya Kano; Philip A Harris; Hideyuki Sato; Ichiro Mori; Rob I West; Megumi Shibahara; Hiroko Toyoda; Liping Wang; Robert T Nolte; James M Veal; Mui Cheung
Journal: J Med Chem Date: 2007-08-04 Impact factor: 7.446

2 in total

1. Evaluation of the Antioxidant Activity of Some Imines Containing 1H-Benzimidazoles.

Authors: Rahman Başaran; Gülgün Kılcıgil; Benay Eke
Journal: Turk J Pharm Sci Date: 2020-12-23

2. New Benzimidazole-, 1,2,4-Triazole-, and 1,3,5-Triazine-Based Derivatives as Potential EGFR^WT and EGFR^T790M Inhibitors: Microwave-Assisted Synthesis, Anticancer Evaluation, and Molecular Docking Study.

Authors: Heba E Hashem; Abd El-Galil E Amr; Eman S Nossier; Manal M Anwar; Eman M Azmy
Journal: ACS Omega Date: 2022-02-18

2 in total

Synthesis and Pharmacologic Evaluation of Some Benzimidazole Acetohydrazide Derivatives as EGFR Inhibitors.

Review 1. The protein kinase complement of the human genome.

2. Design and synthesis of new (E)-cinnamic N-acylhydrazones as potent antitrypanosomal agents.

3. Discovery of novel benzimidazoles as potent inhibitors of TIE-2 and VEGFR-2 tyrosine kinase receptors.

Review 4. Epidermal growth factor receptor (EGFR) signaling in cancer.

5. Novel benzimidazole analogs as inhibitors of EGFR tyrosine kinase.

Review 6. EGFR-TKI resistance in NSCLC patients: mechanisms and strategies.

7. Discovery of benzimidazole derivatives as novel multi-target EGFR, VEGFR-2 and PDGFR kinase inhibitors.

Review 8. Rational bases for the development of EGFR inhibitors for cancer treatment.

1. Evaluation of the Antioxidant Activity of Some Imines Containing 1H-Benzimidazoles.

2. New Benzimidazole-, 1,2,4-Triazole-, and 1,3,5-Triazine-Based Derivatives as Potential EGFR^WT and EGFR^T790M Inhibitors: Microwave-Assisted Synthesis, Anticancer Evaluation, and Molecular Docking Study.

Synthesis and Pharmacologic Evaluation of Some Benzimidazole Acetohydrazide Derivatives as EGFR Inhibitors.

Review 1. The protein kinase complement of the human genome.

2. Design and synthesis of new (E)-cinnamic N-acylhydrazones as potent antitrypanosomal agents.

3. Discovery of novel benzimidazoles as potent inhibitors of TIE-2 and VEGFR-2 tyrosine kinase receptors.

Review 4. Epidermal growth factor receptor (EGFR) signaling in cancer.

5. Novel benzimidazole analogs as inhibitors of EGFR tyrosine kinase.

Review 6. EGFR-TKI resistance in NSCLC patients: mechanisms and strategies.

7. Discovery of benzimidazole derivatives as novel multi-target EGFR, VEGFR-2 and PDGFR kinase inhibitors.

Review 8. Rational bases for the development of EGFR inhibitors for cancer treatment.

1. Evaluation of the Antioxidant Activity of Some Imines Containing 1H-Benzimidazoles.

2. New Benzimidazole-, 1,2,4-Triazole-, and 1,3,5-Triazine-Based Derivatives as Potential EGFRWT and EGFRT790M Inhibitors: Microwave-Assisted Synthesis, Anticancer Evaluation, and Molecular Docking Study.

2. New Benzimidazole-, 1,2,4-Triazole-, and 1,3,5-Triazine-Based Derivatives as Potential EGFR^WT and EGFR^T790M Inhibitors: Microwave-Assisted Synthesis, Anticancer Evaluation, and Molecular Docking Study.