Synthesis and characterisation of novel 2,4-diphenyloxazole derivatives and evaluation of their in vitro antioxidant and anticancer activity

Mathew, Jessy Elizabeth; Divya, G.; Vachala, Seekarajapuram Dinakaran; Mathew, Jesil A; Jeyaprakash, R S

doi:10.1016/j.jopr.2012.12.001

Cited by 3 publications

(2 citation statements)

References 10 publications

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“…In traditional medicine, the underground parts of the plant are rubbed with honey and given to treat leprosy. The roots and stems are used in ethno veterinary aches and pains, rheumatism, anthrax, madness, antibacterial effect, antineoplastic effect, antiarthritic effect and snakebite (Wu et al, 2004;Ramachandran et al, 2008;Sati et al, 2011;Mathew et al, 2011).…”

Section: Original Researchmentioning

confidence: 99%

“…It has been experimentally shown that the plant several various bioactivities such as antimicrobial (Shafi et al, 2002;Umamaheshwari & Muthy, 2012;Venkateswarlu et al, 2013), antioxidant (Thirugnanasampandan et al, 2008;Hossen et al, 2014), inhibition of drug induced hyperuricemia (Ramachandran et al, 2008), anthelmintic (Mini et al, 2013), antihyperglycemic (Shanmugam et al, 2014), antidiarrheal (Dharmalingam et al, 2014), antiinflammatory (Mathew et al, 2011), antipruritic (Mathew et al, 2011), mast cell stabilizing (Mathew et al, 2011) and immunomodulatory (Mallaiah et al, 2015) activity. In the present study, we determined antimicrobial and radical scavenging efficacy of leaf and flower extract of A. indica.…”

Section: Original Researchmentioning

confidence: 99%

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Antimicrobial and Radical Scavenging Efficacy of Leaf and Flower of <i>Aristolochia indica</i> Linn.

Abhishiktha¹,

Saba²,

Shrunga³

et al. 2015

Sci. Technol. Arts Res. J.

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The present study was performed to screen antibacterial, antifungal and radical scavenging efficacy of leaf and flower extract of Antibacterial and antifungal activity was evaluated by agar well diffusion and poisoned food technique respectively. Radical scavenging potential was determined by DPPH free radical scavenging assay. Overall, Leaf extract and flower extract displayed stronger antibacterial and antifungal activity respectively. Leaf extract was found to scavenge DPPH radicals more effectively when compared to flower extract. In suitable form, the plant can be used against microbial infections and oxidative stress.

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Section: Original Researchmentioning

confidence: 99%

Section: Original Researchmentioning

confidence: 99%

Antimicrobial and Radical Scavenging Efficacy of Leaf and Flower of <i>Aristolochia indica</i> Linn.

Abhishiktha¹,

Saba²,

Shrunga³

et al. 2015

Sci. Technol. Arts Res. J.

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Design, synthesis, and insecticidal/acaricidal evaluation of novel pyrimidinamine derivatives containing phenyloxazole moiety

et al. 2019

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Recent Developments in Oxazole Derivatives as Anticancer Agents: Review on Synthetic Strategies, Mechanism of Action and SAR Studies

Kulkarni

Kaur

Jaitak

2022

ACAMC

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Background: Cancer is the world’s third deadliest disease. Despite the availability of numerous treatments, researchers are focusing on the development of new drugs lacking resistance and toxicity issues. Many newly synthesized drugs fail to reach clinical trials due to poor pharmacokinetic properties. Therefore, there is an imperative requisite to expand novel anticancer agents with in vivo efficacy. Objective: This review emphasizes synthetic methods, contemporary strategies used for the inclusion of oxazole moiety, mechanistic targets along with comprehensive structure-activity relationship studies to provide perspective into the rational design of highly efficient oxazole-based anticancer drugs. Methods: Literature related to oxazole derivatives engaged in cancer research is reviewed. This article gives a detailed account of synthetic strategies, targets of oxazole in cancer, including STAT3, Microtubules, G-quadruplex, DNA topoisomerases, DNA damage, Protein kinases, miscellaneous targets, in vitro studies, and some SAR studies. Results : Oxazole derivatives possess potent anticancer activity by inhibiting novel targets such as STAT3 and G-quadruplex. Oxazoles also inhibit tubulin protein to induce apoptosis in cancer cells. Some other targets such as DNA topoisomerase enzyme, protein kinases, and miscellaneous targets including Cdc25, mitochondrial enzymes, HDAC, LSD1, HPV E2 TAD, NQO1, Aromatase, BCl-6, Estrogen receptor, GRP-78, and Keap-Nrf2 pathway are inhibited by oxazole derivatives Many derivatives showed excellent potencies on various cancer cell lines with IC50 values in nanomolar concentrations. Conclusion: Oxazole is a five-membered heterocycle, with oxygen and nitrogen at 1 and 3 positions respectively. It is often combined with other pharmacophores in the expansion of novel anticancer drugs. In summary, oxazole is a promising entity to develop new anticancer drugs.

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Synthesis and characterisation of novel 2,4-diphenyloxazole derivatives and evaluation of their in vitro antioxidant and anticancer activity

Cited by 3 publications

References 10 publications

Antimicrobial and Radical Scavenging Efficacy of Leaf and Flower of <i>Aristolochia indica</i> Linn.

Antimicrobial and Radical Scavenging Efficacy of Leaf and Flower of <i>Aristolochia indica</i> Linn.

Design, synthesis, and insecticidal/acaricidal evaluation of novel pyrimidinamine derivatives containing phenyloxazole moiety

Recent Developments in Oxazole Derivatives as Anticancer Agents: Review on Synthetic Strategies, Mechanism of Action and SAR Studies

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