Synthesis of new coumarin tethered isoxazolines as potential anticancer agents

Lingaraju, Gejjalagere S.; Balaji, K.; Jayarama, Shankar; Anil, Seegehalli M; Kiran, Kuppalli R.; Sadashiva, M. P.

doi:10.1016/j.bmcl.2018.10.046

Cited by 46 publications

(12 citation statements)

References 51 publications

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“…Only one derivative with a 3,4-dimethoxy substitution did not show any cytotoxicity against a normal fibroblast cell line (FF2441) in the same concentration range. These results were corroborated in the Ehrlich ascites carcinoma animal model, highlighting significantly lowered cell viability, body weight, ascites volume as well as a down-regulation of angiogenesis and tumor growth [134].…”

Section: Coumarin and Angiogenesis Inhibitionmentioning

confidence: 69%

Antiangiogenic Effects of Coumarins against Cancer: From Chemistry to Medicine

et al. 2019

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Angiogenesis, the process of formation and recruitment of new blood vessels from pre-existing vessels, plays an important role in the development of cancer. Therefore, the use of antiangiogenic agents is one of the most critical strategies for the treatment of cancer. In addition, the complexity of cancer pathogenicity raises the need for multi-targeting agents. Coumarins are multi-targeting natural agents belonging to the class of benzopyrones. Coumarins have several biological and pharmacological effects, including antimicrobial, antioxidant, anti-inflammation, anticoagulant, anxiolytic, analgesic, and anticancer properties. Several reports have shown that the anticancer effect of coumarins and their derivatives are mediated through targeting angiogenesis by modulating the functions of vascular endothelial growth factor as well as vascular endothelial growth factor receptor 2, which are involved in cancer pathogenesis. In the present review, we focus on the antiangiogenic effects of coumarins and related structure-activity relationships with particular emphasis on cancer.

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Section: Coumarin and Angiogenesis Inhibitionmentioning

confidence: 69%

Antiangiogenic Effects of Coumarins against Cancer: From Chemistry to Medicine

et al. 2019

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“…Natural and synthetic coumarins (2H-chromen-2-one) demonstrate diverse biological activities, and are often considered as a privileged scaffold [1][2][3][4][5][6]. In particular, a large number of coumarin derivatives with high antitumor activity have been found in recent years [7][8][9][10][11][12][13][14][15][16][17][18]. Natural derivatives of 7-hydroxycoumarin containing terpene fragments have also attracted the attention of the medicinal chemistry community [19][20][21].…”

Section: Introductionmentioning

confidence: 99%

Promising New Inhibitors of Tyrosyl-DNA Phosphodiesterase I (Tdp 1) Combining 4-Arylcoumarin and Monoterpenoid Moieties as Components of Complex Antitumor Therapy

Khomenko

Zakharenko

Chepanova

et al. 2019

IJMS

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Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is an important DNA repair enzyme in humans, and a current and promising inhibition target for the development of new chemosensitizing agents due to its ability to remove DNA damage caused by topoisomerase 1 (Top1) poisons such as topotecan and irinotecan. Herein, we report our work on the synthesis and characterization of new Tdp1 inhibitors that combine the arylcoumarin (neoflavonoid) and monoterpenoid moieties. Our results showed that they are potent Tdp1 inhibitors with IC50 values in the submicromolar range. In vivo experiments with mice revealed that compound 3ba (IC50 0.62 µM) induced a significant increase in the antitumor effect of topotecan on the Krebs-2 ascites tumor model. Our results further strengthen the argument that Tdp1 is a druggable target with the potential to be developed into a clinically-potent adjunct therapy in conjunction with Top1 poisons.

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“…The crude Phloem exudate/sap samples (10 µg/CAM) was treated on the growing CAM by making a small window on the eggshell as described earlier. 23,24 The windows were opened on the 12th day and inspected for changes in the microvessel density and photographed using a Nikon Digital camera.…”

Section: In-ovo Cam Angiogenesis Assaymentioning

confidence: 99%

Screening and Evaluation of Lectin and Anti-Cancer Activity from the Phloem Exudate/Sap of the Indian Dietary Ethnomedicinal Plants

Srinivas¹,

Shivamadhu²,

Devegowda³

et al. 2019

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Objective: Lectins are extremely significant biomolecules to study several biological progressions. In this present investigation, we are screening the crude phloem exudate/ sap sample from different ethnomedicinal plants were evaluated for lectin and anticancer activity. Methods: The lectin activity of crude phloem exudate/sap samples were confirmed by haemgglutination assay and anticancer activity by using trypan blue, MTT and in-ovo CAM angiogenic assay. The tumor cell nuclei resulting in Giemsa stain, AO/EtBr stain, DNA Fragmentation and Caspase-3 inhibitor assay. Results: Our experimental data show that the phloem exudate/sap sample S2 (Musa acuminata), sample S4 (Euphorbia geniculate) exerting the potent lectin activity, sample S5 exerting very low lectin activity against the trypsinized rabbit erythrocytes and decreases the cell viability in EAC cells in-vitro. Sample S2, S4 and S5 exerts significant cytotoxic effect against the various human cancer cell lines and regressed the neovasculature (development of new blood vessels) in the developing CAM embryos when compared to the other crude samples. The apoptotic inducing activity of crude phloem exudate/sap samples was revealed by DNA fragmentation assay, caspase-3 inhibitor assay and cellular morphology were studied by fluorescence staining methods. Conclusion: This study reports that some of the isolated crude phloem exudate/sap samples show potent lectin activity and anti-cancer activity in different human cancer cell lines. The further additional experiment needs to purify and characterize the bioactive lectin components from the potent sample which is responsible for pro-apoptotic, anti-angiogenic activity and mechanism involved.

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Synthesis of new coumarin tethered isoxazolines as potential anticancer agents

Cited by 46 publications

References 51 publications

Antiangiogenic Effects of Coumarins against Cancer: From Chemistry to Medicine

Antiangiogenic Effects of Coumarins against Cancer: From Chemistry to Medicine

Promising New Inhibitors of Tyrosyl-DNA Phosphodiesterase I (Tdp 1) Combining 4-Arylcoumarin and Monoterpenoid Moieties as Components of Complex Antitumor Therapy

Screening and Evaluation of Lectin and Anti-Cancer Activity from the Phloem Exudate/Sap of the Indian Dietary Ethnomedicinal Plants

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