Antiproliferative activity and p53 upregulation effects of chalcones on human breast cancer cells

Santos, Mariana Bastos dos; Anselmo, Daiane Bertholin; Oliveira, J.G.; Jardim‐Perassi, Bruna V.; Monteiro, Diego Alves; Silva, Gabriel; Gomes, Eleni; Fachin, Ana Lúcia; Marins, Mozart; Zuccari, Débora Aparecida Pires de Campos; Regasini, Luis Octávio

doi:10.1080/14756366.2019.1615485

Cited by 42 publications

(48 citation statements)

References 47 publications

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“…The anticancer activity of 4′-amino-1-naphthyl- chalcone and 4′-amino-4-methyl-1-naphthylchalcone described by Seba et al proved the ability of these derivatives to inhibit the migration and invasion of osteosarcoma cells, especially in p53-expressing cells (U2OS) [22]. Moreover, Santos et al showed that aminochalcones containing a fluorine atom at the C-2 position and a pyridyl group at the C-3 position induced apoptosis due to upregulated p53 protein expression in the breast cancer cell lines MCF-7 (ER) and MDA-MB-231 (TNBC) [23]. The studies of Pati et al proved that incorporation of an amino moiety into the ring B of the methoxychalcones may increase their cytotoxicity against a murine melanoma cell line (B16) with the effect depending on the location of the substituent [10].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Evaluation of Novel Aminochalcones as Potential Anticancer and Antimicrobial Agents

et al. 2019

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A series of 18 aminochalcone derivatives were obtained in yields of 21.5–88.6% by applying the classical Claisen-Schmidt reaction. Compounds 4–9, 14 and 16–18 with 4-ethyl, 4-carboxy-, 4-benzyloxy- and 4-benzyloxy-3-methoxy groups were novel, not previously described in the scientific literature. To determine the biological properties of the synthesized compounds, anticancer and antimicrobial activity assays were performed. Antiproliferative potential was evaluated on four different human colon cancer cell lines—HT-29, LS180, LoVo and LoVo/DX —using the SRB assay and compared with green monkey kidney fibroblasts COS7. Anticancer activity was described as the IC50 value. The best results were observed for 2′-aminochalcone (1), 3′-aminochalcone (2) and 4′-aminochalcone (3) (IC50 = 1.43–1.98 µg·mL−1) against the HT-29 cell line and for amino-nitrochalcones 10–12 (IC50 = 2.77–3.42 µg·mL−1) against the LoVo and LoVo/DX cell lines. Moreover, the antimicrobial activity of all derivatives was evaluated on two strains of bacteria: Escherichia coli ATCC10536 and Staphylococcus aureus DSM799, the yeast strain Candida albicans DSM1386 and three strains of fungi: Alternaria alternata CBS1526, Fusarium linii KB-F1 and Aspergillus niger DSM1957. In the case of E. coli ATCC10536 almost all derivatives hindered the bacterial growth (∆OD = 0). Furthermore, the best results were observed in the presence of 4′-aminochalcone (3), that completely limited the growth of all tested strains at the concentration range of 0.25–0.5 mg·mL−1. The strongest bacteriostatic activity was exhibited by novel 3′-amino-4-benzyloxychalcone (14), that prevented the growth of E. coli ATCC10536 with MIC = 0.0625 mg·mL−1.

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Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Evaluation of Novel Aminochalcones as Potential Anticancer and Antimicrobial Agents

et al. 2019

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“…Due to their various biological and pharmacological properties, chalcones and its derivatives are intensely involved in the medicinal and industrial aspects [ 81 ]. Natural and synthetic chalcones exhibit a wide variety of biological properties including anti-proliferative [ 82 ], anti-inflammatory [ 83 ], anti-cancer [ 84 ], anti-tubercular and anti-bacterial [ 85 ], anti-fungal [ 86 ], anti-oxidant [ 87 ] and anti-leishmanial activities [ 88 ]. In addition, naturally occurring chalcones are precursors in the biosynthesis of chromanones and flavanones and play a significant role in the plant protection against ultraviolet radiation, diseases and insects [ 89 ].…”

Section: An Overview Of Chalcones Derivatives As Possible Therapeuticmentioning

confidence: 99%

Recent investigations into synthesis and pharmacological activities of phenoxy acetamide and its derivatives (chalcone, indole and quinoline) as possible therapeutic candidates

2021

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Graphical abstract Medicinal chemistry can rightfully be regarded as a cornerstone in the public health of our modern society that combines chemistry and pharmacology with the aim of designing and developing new pharmaceutical compounds. For this purpose, many chemical techniques as well as new computational chemistry applications are used to study the utilization of drugs and their biological effects. In the biological interface, medicinal chemistry constitutes a group of interdisciplinary sciences, as well as controlling its organic, physical and computational pillars. Therefore, medicinal chemists working to design an integrated and developing system that portends an era of novel and safe tailored drugs either by synthesizing new pharmaceuticals or to improving the processes by which existing pharmaceuticals are made. It includes researching the effects of synthetic, semi-synthetic and natural biologically active substances based on molecular interactions in terms of molecular structure with triggered functional groups or the specific physicochemical properties. The present work focuses on the literature survey of chemical diversity of phenoxy acetamide and its derivatives (Chalcone, Indole and Quinoline) in the molecular framework in order to get complete information regarding pharmacologically interesting compounds of widely different composition. From a biological and industrial point of view, this literature review may provide an opportunity for the chemists to design new derivatives of phenoxy acetamide and its derivatives that proved to be the successful agent in view of safety and efficacy to enhance life quality.

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“…Moreover mechanisms of action of bioactive compounds isolated from A. pindrow also needs to be further explored for clarity of pharmacological actions. There has been reports from various studies that chalcones behave as strong antioxidants [69,70] and antiproliferative activities [71,72]. Since chalcones have been isolated from the barks of A. pindrow, investigations on anticancer and antiproliferative activity also needs to be undertaken for development of anticancer drug.…”

Section: Conclusion and Future Prospectsmentioning

confidence: 99%

Ethnobotanical and Pharmacological Importance of Western Himalayan Fir Abies pindrow (Royle ex D. Don) Royle: A Review

Sinha¹

2019

JPRI

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Aims: Abies pindrow (Royle ex D. Don) Royle., colloquially known as the Western Himalayan fir, is a conifer that grows along the Himalayan mountains from Afghanistan to Nepal. The plant is extensively used by locals for the treatments of various ailments. Thus based on the available reports about its importance in traditional system of medicine, an attempt has been made to review this species in context of its medicinal and pharmaceutical importance. Study Design: The review article has been designed based on literature survey. The article is grossly divided into four broad phases consisting of compiled information of Abies pindrow: (1) Ethnobotanical information (2) Chemical Constituents (3) Pharmacological activities (4) Discussion mainly highlighting the mode of action of the bioactive compounds in relation to its pharmacological activity. Methodology: Extensive literature search have been performed in the web using PubMed, PubMed Central, google scholar as search platform. Efforts have also been taken to compile information from research papers and review articles not more than 10 years old. Information from old literatures were preferably avoided unless found to be very relevant to the subject. Results: The literature survey revealed that the plant has been used to treat cough and cold, diabetes, cataract and bladder diseases. The plant is also considered to be carminative, astringent, antispasmodic, diuretic, tonic and anti-inflammatory. The plant is also rich in terpenes and terpene alcohols. Testing for antidiabetic, neuroprotective, anticataract and antixiolytic activities have been promising and the bioactive constituents and efforts are made to interpret the possible mechanism of action of bioactive compounds in bringing about the pharmacological activities. Conclusion: It is concluded that the plant can be explored and bioprospected for an affordable source of drug and nutraceutical for better management of health related issues of people of Indian subcontinent.

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Antiproliferative activity and p53 upregulation effects of chalcones on human breast cancer cells

Cited by 42 publications

References 47 publications

Synthesis and Biological Evaluation of Novel Aminochalcones as Potential Anticancer and Antimicrobial Agents

Synthesis and Biological Evaluation of Novel Aminochalcones as Potential Anticancer and Antimicrobial Agents

Recent investigations into synthesis and pharmacological activities of phenoxy acetamide and its derivatives (chalcone, indole and quinoline) as possible therapeutic candidates

Ethnobotanical and Pharmacological Importance of Western Himalayan Fir Abies pindrow (Royle ex D. Don) Royle: A Review

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