Antiproliferative activity, enzymatic inhibition and apoptosis-promoting effects of benzoxazole-based hybrids on human breast cancer cells

Omar, Ashraf M.; Aboulwafa, Omaima M.; Amr, Mai E.; El-Shoukrofy, Mai S.

doi:10.1016/j.bioorg.2021.104752

Cited by 20 publications

(18 citation statements)

References 55 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Compounds 43a , 43b , 44b and 44d ( Figure 3 ) had an inhibitory effect on MDA-MB-231 cells. The inhibitory effect was stronger than that of Doxorubicin, with IC 50 values of 0.59 ± 0.02, 3.59 ± 0.2, 1.24 ± 0.06 and 1.16 ± 0.04 µM, respectively 50 .…”

Section: Oxadiazolementioning

confidence: 85%

Research progress on the synthesis and pharmacology of 1,3,4-oxadiazole and 1,2,4-oxadiazole derivatives: a mini review

Wang

Sun

Jia

et al. 2022

Journal of Enzyme Inhibition and Medicinal Chemistry

View full text Add to dashboard Cite

Oxadiazole is a five-membered heterocyclic compound containing two nitrogen atoms and one oxygen atom. The 1,3,4-oxadiazole and 1,2,4-oxadiazole have favourable physical, chemical, and pharmacokinetic properties, which significantly increase their pharmacological activity via hydrogen bond interactions with biomacromolecules. In recent years, oxadiazole has been demonstrated to be the biologically active unit in a number of compounds. Oxadiazole derivatives exhibit antibacterial, anti-inflammatory, anti-tuberculous, anti-fungal, anti-diabetic and anticancer activities. In this paper, we report a series of compounds containing oxadiazole rings that have been published in the last three years only (2020–2022) as there was no report or their activities described in any article in 2019, which will be useful to scientists in research fields of organic synthesis, medicinal chemistry, and pharmacology.

show abstract

Section: Oxadiazolementioning

confidence: 85%

Research progress on the synthesis and pharmacology of 1,3,4-oxadiazole and 1,2,4-oxadiazole derivatives: a mini review

Wang

Sun

Jia

et al. 2022

Journal of Enzyme Inhibition and Medicinal Chemistry

View full text Add to dashboard Cite

show abstract

“…To check apoptosis potential, caspase-9 activation assay was performed, where MCF-7 cell lines were treated with compounds 23 and derivatives and exhibited significant increase in its concentration (23.91 � 2.43 ng/mL). [52] Liangkun et al π-σ interactions and hydrophobic interactions. Structure-activity relationship study concluded that trimethoxy phenyl substitution is essential for anticancer activity.…”

Section: Triazole Fused With Thiadiazine/thiadiazolmentioning

confidence: 99%

Synthetic and Medicinal Perspective of 1,2,4‐Triazole as Anticancer Agents

Rathod

Kumar

2022

Chemistry & Biodiversity

View full text Add to dashboard Cite

Cancer is still one of the leading causes of death worldwide. Many researchers are working to design and develop heterocyclic-based drugs with the potential to treat cancer at various stages. There is always an unmet need to discover new anticancer drugs to treat different types of cancer. Based on literature reports, it was evident that hybrid 1,2,4-triazoles exhibit a wide spectrum of biological potential (particularly potent anticancer activity), as compared to the corresponding monocyclic compounds. In this review, we summarized fused/hybrid 1,2,4-triazole and poly-functionalized 1,2,4-triazoles as anticancer agents. Triazole may be fused with other heterocyclic scaffolds like pyrimidine, pyridine, piperidine, quinoxaline, quinazoline, thiadiazine, indole, phthalazine etc. A clear explanation of the method of synthesis, structure-activity relationship, and in vitro results plus the inhibitory concentration of new molecules are focused on in this review article.

show abstract

“… 17 Some 1,2,4-triazolo[3,4- b ]thiadiazine scaffolds had promising anticancer activities against several human cancer cell lines without obvious signs of toxicity. 18–24 Interestingly, a list of triazole, thiadiazole and quinoxaline-based compounds with promising EGFR and PARP-1 inhibition is described in Fig. 2 , hence, we thought to employ these moieties as an approach of fragment-based drug design.…”

Section: Introductionmentioning

confidence: 99%

Design and synthesis of new bis(1,2,4-triazolo[3,4-b][1,3,4]thiadiazines) and bis((quinoxalin-2-yl)phenoxy)alkanes as anti-breast cancer agents through dual PARP-1 and EGFR targets inhibition

et al. 2022

View full text Add to dashboard Cite

show abstract

Antiproliferative activity, enzymatic inhibition and apoptosis-promoting effects of benzoxazole-based hybrids on human breast cancer cells

Cited by 20 publications

References 55 publications

Research progress on the synthesis and pharmacology of 1,3,4-oxadiazole and 1,2,4-oxadiazole derivatives: a mini review

Research progress on the synthesis and pharmacology of 1,3,4-oxadiazole and 1,2,4-oxadiazole derivatives: a mini review

Synthetic and Medicinal Perspective of 1,2,4‐Triazole as Anticancer Agents

Design and synthesis of new bis(1,2,4-triazolo[3,4-b][1,3,4]thiadiazines) and bis((quinoxalin-2-yl)phenoxy)alkanes as anti-breast cancer agents through dual PARP-1 and EGFR targets inhibition

Contact Info

Product

Resources

About