Journal ArticleDOI
Design, synthesis, antiproliferative evaluation, and molecular docking study of new quinoxaline derivatives as apoptotic inducers and EGFR inhibitors
Eman A. Fayed,Yousry A. Ammar,Marwa A. Saleh,Ashraf H. Bayoumi,Amany Belal,Amany Belal,Ahmed B.M. Mehany,Ahmed Ragab +7 more
TLDR
A new series of quinoxaline derivatives synthesized and pharmacologically evaluated against (HepG-2, HCT-116, and MCF-7) cell lines and revealed that it increases apoptotic cells and induced cell cycle arrest at pre-G1 and G2/M phases.About:
This article is published in Journal of Molecular Structure.The article was published on 2021-07-15. It has received 39 citations till now. The article focuses on the topics: Quinoxaline.read more
Citations
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Hydrazonoyl bromide precursors as DHFR inhibitors for the synthesis of bis-thiazolyl pyrazole derivatives; antimicrobial activities, antibiofilm, and drug combination studies against MRSA.
TL;DR: In this article, a series of new bis-thiazolyl-pyrazole derivatives 3, 4a-c, 5a, b, and 6a -c was synthesized by reacting bis hydrazonoyl bromide with several active methylene reagents in a one-pot reaction.
Journal ArticleDOI
Design, synthesis of new magenta dyestuffs based on thiazole azomethine disperse reactive dyes with antibacterial potential on both dyes and gamma-irradiated dyed fabric
TL;DR: In this paper, a series of new magenta azomethine reactive disperse dyes were synthesized and applied into polyester/cotton blend fabrics, and various spectroscopic and analytical techniques characterized all the synthesized dyes.
Journal ArticleDOI
Development of novel indolin-2-one derivative incorporating thiazole moiety as DHFR and quorum sensing inhibitors: Synthesis, antimicrobial, and antibiofilm activities with molecular modelling study
TL;DR: In this paper , a series of new thiazolo-indolin-2-one derivatives were synthesized based on acid and base catalyzed condensation or reaction of thiosemicarbazone 8 with different electrophilic reagents.
Journal ArticleDOI
One-Pot Synthesis and Molecular Modeling Studies of New Bioactive Spiro-Oxindoles Based on Uracil Derivatives as SARS-CoV-2 Inhibitors Targeting RNA Polymerase and Spike Glycoprotein
Samar A. El-Kalyoubi,Ahmed Ragab,Ola A. Abu Ali,Yousry A. Ammar,Mohamed G. Seadawy,Aya Ahmed,Eman A. Fayed +6 more
TL;DR: This study aims to design a simple and efficient cyclo-condensation reaction of 6-aminouracil derivatives 2a–e and isatin derivatives 1a–c to synthesize spiro-oxindoles 3a–d, 4 a–e, and 5a-e to synthesise spiro’s most active hybrids.
Journal ArticleDOI
Design, synthesis of new novel quinoxalin-2(1H)-one derivatives incorporating hydrazone, hydrazine, and pyrazole moieties as antimicrobial potential with in-silico ADME and molecular docking simulation
Ahmed Ragab,Doaa M. Elsisi,Ola A. Abu Ali,Moustafa S. Abusaif,Ahmed A. Askar,Awatef A. Farag,Yousry A. Ammar +6 more
TL;DR: A series of 6-(morpholinosulfonyl)quinoxalin-2(1H)-one based hydrazone, hydrazine, and pyrazole moieties were designed, synthesized, and evaluated for their in vitro antimicrobial activity.
References
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Journal ArticleDOI
Cancer statistics, 2016
TL;DR: Overall cancer incidence trends are stable in women, but declining by 3.1% per year in men, much of which is because of recent rapid declines in prostate cancer diagnoses, and brain cancer has surpassed leukemia as the leading cause of cancer death among children and adolescents.
Journal ArticleDOI
Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
TL;DR: Experimental and computational approaches to estimate solubility and permeability in discovery and development settings are described in this article, where the rule of 5 is used to predict poor absorption or permeability when there are more than 5 H-bond donors, 10 Hbond acceptors, and the calculated Log P (CLogP) is greater than 5 (or MlogP > 415).
Journal ArticleDOI
Bcl-2 heterodimerizes in vivo with a conserved homolog, Bax, that accelerates programed cell death
TL;DR: Overexpressed Bax accelerates apoptotic death induced by cytokine deprivation in an IL-3-dependent cell line and counters the death repressor activity of B cl-2, suggesting a model in which the ratio of Bcl-2 to Bax determines survival or death following an apoptotic stimulus.
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The BCL-2 protein family: opposing activities that mediate cell death
TL;DR: New insights into interactions among BCL-2 family proteins reveal how these proteins are regulated, but a unifying hypothesis for the mechanisms they use to activate caspases remains elusive.
Journal ArticleDOI
Sulforhodamine B colorimetric assay for cytotoxicity screening
TL;DR: The sulforhodamine B (SRB) assay is used for cell density determination, based on the measurement of cellular protein content, which is an efficient and highly cost-effective method for screening.