4 research outputs found

    Anticancer Functions of Pyridine Heterocycles

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    Pyridine is a heterocyclic molecule with a nitrogen atom that is often found in nature. As a prosthetic group taking part in redox processes in the biological system, it plays an important function in many enzymes of the living system. Pyridine is an important pharmacophore, a privileged scaffold, and a superior heterocyclic system in drug development, with various applications in anticancer research because of its ability to work on significant receptors. Typically, it is the core of several currently available medicines. In the fight against cancer, many pyridine derivatives have been shown to inhibit kinases, androgen receptors, tubulin polymerization, topoisomerase enzyme, human carbonic anhydrase, and several other targets. Researchers are now concentrating on developing pyridine novel entities with other moieties for cancer therapy. This section presents pyridine derivative synthesis and biological expansions, as well as their target receptor sites

    1,2,3-Triazole-Containing Compounds as Anti–Lung Cancer Agents: Current Developments, Mechanisms of Action, and Structure–Activity Relationship

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    Lung cancer is the most common malignancy and leads to around one-quarter of all cancer deaths. Great advances have been achieved in the treatment of lung cancer with novel anticancer agents and improved technology. However, morbidity and mortality rates remain extremely high, calling for an urgent need to develop novel anti–lung cancer agents. 1,2,3-Triazole could be readily interact with diverse enzymes and receptors in organisms through weak interaction. 1,2,3-Triazole can not only be acted as a linker to tether different pharmacophores but also serve as a pharmacophore. This review aims to summarize the recent advances in 1,2,3-triazole–containing compounds with anti–lung cancer potential, and their structure–activity relationship (SAR) together with mechanisms of action is also discussed to pave the way for the further rational development of novel anti–lung cancer candidates

    Anti-angiogenic and toxicity effects of Derris trifoliata extract in zebrafish embryo

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    Introduction: Derris trifoliata has been traditionally used as folk for the treatment of , rheumatic joints, diarrhoea, and dysmenorrhea, and rotenoids isolated from the plant have shown to exhibit anti-cancer properties. This study aimed to assess the toxicity effects and antiangiogenic activity of extract of Derris trifoliata on zebrafish embryo model. Materials and Methods: Zebrafihs embryos were treated with aqueous extract of Derris Trifoliata to evaluate its effects on angiogenesis and zebrafish-toxicity. Angiogenic response was analyzed using whole-mount alkaline phosphatase (AP) vessel staining on 72 hours post fertilization (hpf) zebrafish embryos. Results: 1.0 mg/ml concentration was toxic to zebrafish embryos and embryos exposed to concentrations at 0.5 mg/ml and below showed some malformations. Derris trifoliata aqueous extract also showed some anti-angiogenic activity in vivo in the zebrafish embryo model wereby at high concentration inhibited vessel formation in zebrafish embryo. Conclusions: The anti-angiogenic response of extract of Derris trifoliata in zebrafish in vivo model suggest its therapeutic potential as anti-cancer agent
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