New pyrimidine-benzoxazole/benzimidazole hybrids: Synthesis, antioxidant, cytotoxic activity, in vitro cyclooxygenase and phospholipase A2-V inhibition

Abdelgawad, Mohamed A.; Bakr, Rania B.; Ahmad, Waqas; Al-Sanea, Mohammad M.; Elshemy, Heba A.H.

doi:10.1016/j.bioorg.2019.103218

Cited by 56 publications

(27 citation statements)

References 29 publications

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“…Additionally, derivative (24b) displayed two hydrogen bonds; (1) C]O with Gln192 (2.79Å), and (2) C]O with Arg513 (2.51Å). 81 New pyrimidine-pyridine hybrids (Fig. 10) have also been reported for their potential use as anti-inammatory candidates.…”

Section: Cyclooxygenase Inhibitionmentioning

confidence: 99%

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Research developments in the syntheses, anti-inflammatory activities and structure–activity relationships of pyrimidines

et al. 2021

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Section: Cyclooxygenase Inhibitionmentioning

confidence: 99%

“…noticed to be equipotent to diclofenac-sodium. The IC 50 values of compounds(81)(82)(83)(84)(85) were recorded to be 143.26 mmol kg À1 , 130.44 mmol kg À1 , 114.03 mmol kg À1 , 83.36 mmol kg À1 , and 81.31 mmol kg À1 , respectively as compared to diclofenacsodium (IC 50 ¼ 141.03 mmol kg À1…”

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confidence: 99%

Research developments in the syntheses, anti-inflammatory activities and structure–activity relationships of pyrimidines

et al. 2021

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“…The compounds 51 a – c , 52 , and 53 exhibited good activity and more selectivity against cell lines, and 53 exerted potent cytotoxic activity with IC 50 value 4.14 μM against A‐549 cell (Figure 19). [67] …”

Section: Imidazole Hybridizes With Other Anticancer Pharmacophoresmentioning

confidence: 99%

Hybridization of Imidazole with Various Heterocycles in Targeting Cancer: A Decade's Work

Teli¹,

Chawla²

2021

ChemistrySelect

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Cancer is the world‘s biggest global health concern. The prevalence and mortality rates of cancer remain high despite significant progress in cancer therapy. The search for more effective, as well as less toxic treatment methods for cancer, is at the focus of current studies. Approximately 24.6 million people are suffering from cancer across the world as per the world health organization (WHO). In the year 2020, approximately 10 million deaths were reported due to cancer which has emerged as the second leading cause of mortality across the globe. Anticancer medicines have played a pivotal role in the medication of different types of cancers; however, they are associated with several side effects and relevance of drug resistance which evoke an immediate need for designing of new anticancer agents with multitargeted effect. Imidazole is a heterocyclic compound privileged with considerable anticancer activities and some imidazole derivatives have already got approval to treat cancer. Many hybrid molecules are available that play an important role in the treatment of cancer like chalcone, pyrazole, purine, triazine etc., and their pharmacophore provide the anticancer drug with low drug resistance and high efficacy, with low chances of toxicity and side effects. This review provides various approaches for the drug development of new safe and efficient antitumor agents imidazole hybrids with other heterocyclic moieties. An attempt has been made to advancement of the anticancer potential of the derivatives and hybrids of imidazole having intact or condensed imidazole moiety in the last decade along with the structure‐activity relationship studies, and mechanism of action.

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“…Pyrimidine moiety has shown anticancer activity previously, so new series of Benzoxazole azo-pyrimidine [61] and benzimidazole azo-pyrimidine were synthesized by using very simple steps. Firstly, the 3-aminophenyl benzoxazole and benzimidazole were synthesized, and then, they were made into diazonium salt and coupled with diethyl malonate further this intermediate was cyclised with urea to prepare new variety of pyrimidine benzoxazole and benzimidazole hybrids (Fig.…”

Section: Benzoxazole-pyrimidine Derivativementioning

confidence: 99%

Anticancer activity of benzoxazole derivative (2015 onwards): a review

Ghoshal

Patel

2020

Futur J Pharm Sci

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Background According to the report published recently by the World Health Organization, the number of cancer cases in the world will increase to 22 million by 2030. So the anticancer drug research and development is taking place in the direction where the new entities are developed which are low in toxicity and are with improved activity. Benzoxazole and its derivative represent a very important class of heterocyclic compounds, which have a diverse therapeutic area. Recently, many active compounds synthesized are very effective; natural products isolated with benzoxazole moiety have also shown to be potent towards cancer. Main text In the last few years, many research groups have designed and developed many novel compounds with benzoxazole as their backbone and checked their anticancer activity. In the review article, the recent developments (mostly after 2015) made in the direction of design and synthesis of new scaffolds with very potent anticancer activity are briefly described. The effect of various heterocycles attached to the benzoxazole and their effect on the anticancer activity are thoroughly studied and recorded in the review. Conclusion These compiled data in the article will surely update the scientific community with the recent development in this area and will provide direction for further research in this area.

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New pyrimidine-benzoxazole/benzimidazole hybrids: Synthesis, antioxidant, cytotoxic activity, in vitro cyclooxygenase and phospholipase A2-V inhibition

Cited by 56 publications

References 29 publications

Research developments in the syntheses, anti-inflammatory activities and structure–activity relationships of pyrimidines

Research developments in the syntheses, anti-inflammatory activities and structure–activity relationships of pyrimidines

Hybridization of Imidazole with Various Heterocycles in Targeting Cancer: A Decade's Work

Anticancer activity of benzoxazole derivative (2015 onwards): a review

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