Novel structural hybrids of quinoline and thiazole moieties: Synthesis and evaluation of antibacterial and antifungal activities with molecular modeling studies

Eissa, Sally I.; Farrag, Ayman A.; Abbas, Samir Y.; Shehry, Mohamed F. El; Ragab, Ahmed; Fayed, Eman A.; Ammar, Yousry A.

doi:10.1016/j.bioorg.2021.104803

Cited by 72 publications

(30 citation statements)

References 39 publications

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“…Amides thus play an important part in essential life processes, because the amide bond is, for example, the key to the production of proteins. In addition, amide bond is commonly used in the structure of 25% of the well-known drugs, according to the Comprehensive Medicinal Chemistry database [25,26].…”

Section: Introducionmentioning

confidence: 99%

Carboxamide appended quinoline moieties as potential anti-proliferative agents, apoptotic inducers and Pim-1 kinase inhibitors

et al. 2021

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The targeted approach of protein kinases (PKs), as PKs are the main regulators of cell survival and proliferation, has been a promising strategy for treatments for cancer. Here we analyze the potential of quinoline-carboximide derivatives for four cell lines: MCF-7, CACO, HepG-2 and HCT-116 as anticancer agents. 3e, 4b, 11b and 13d derivatives showed good anti-proliferative activities in comparison to the reference standard Doxorubicin, against the four cell lines tested. They have been chosen for further studies. First of all, the IC50 value surveys were carried out to ensure the protection of our hits and demonstrate that the cytotoxic effect (IC50 > 113 μM) is highly selective on normal human cells (WI-38). Secondly, apoptosis was accomplished by down-regulation of Bcl-2 and up-regulation of BAX and Caspase-3 by these active compounds. Also, the Pim-1 inhibitory activity of the active hybrids was done, which indicate that compound 3e was the most active with percentage of inhibition 82.27% and IC50 equal 0.11 when compaired to SGI-1776 as a reference standered. In addition, the in silico assessment of ADME properties, all of the strongest compounds are orally bioavailable without blood brain barrier penetration.

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Section: Introducionmentioning

confidence: 99%

Carboxamide appended quinoline moieties as potential anti-proliferative agents, apoptotic inducers and Pim-1 kinase inhibitors

et al. 2021

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“…For example, PDF has been identified as a promising drug target against several human pathogens including Mpn [108] . Although no PDF inhibitor is currently on the market [109] , this metalloenzyme is the subject of numerous active investigations [110] , [111] . In these efforts, homology modeling, combined with additional in silico methods, could provide valuable information in the structure-based druggability assessment of a specific target [112] .…”

Section: Discussionmentioning

confidence: 99%

Metal utilization in genome-reduced bacteria: Do human mycoplasmas rely on iron?

Perálvarez-Marín

Baranowski²,

Bierge³

et al. 2021

Computational and Structural Biotechnology Journal

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“…Recently, quinolones/quinolones and thiazole derivatives are known for their strong antimicrobial effect and displayed good antibacterial activity [50,51]. In contrast, the literature reports reveal that the α-aminophosphonates derivatives displayed good and promising antimicrobial activity [49].…”

Section: Antimicrobial Activitymentioning

confidence: 99%

Synthesis and potential antimicrobial activity of novel α-aminophosphonates derivatives bearing substituted quinoline or quinolone and thiazole moieties

et al. 2021

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Novel structural hybrids of quinoline and thiazole moieties: Synthesis and evaluation of antibacterial and antifungal activities with molecular modeling studies

Cited by 72 publications

References 39 publications

Carboxamide appended quinoline moieties as potential anti-proliferative agents, apoptotic inducers and Pim-1 kinase inhibitors

Carboxamide appended quinoline moieties as potential anti-proliferative agents, apoptotic inducers and Pim-1 kinase inhibitors

Metal utilization in genome-reduced bacteria: Do human mycoplasmas rely on iron?

Synthesis and potential antimicrobial activity of novel α-aminophosphonates derivatives bearing substituted quinoline or quinolone and thiazole moieties

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