Antitumor potential of 1-thiocarbamoyl-3,5-diaryl-4,5-dihydro-1H-pyrazoles in human bladder cancer cells

Tessmann, Josiane Weber; Buss, Julieti H.; Begnini, Karine R.; Berneira, Lucas M.; Paula, Fávero Reisdorfer; Pereira, Cláudio Martin Pereira de; Collares, Tiago; Seixas, Fabiana Kömmling

doi:10.1016/j.biopha.2017.07.060

Cited by 33 publications

(14 citation statements)

References 59 publications

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“…Some compounds were active against the tested cell lines having low IC 50 values with compound (14) as the best candidate in this series. Potential antitumor performance of 1-thiocarbamoyl-3,5-diaryl-4,5-dihydro-1H-pyrazole derivatives were studied by Tessmann et al 13 . Two human bladder cancer cell lines 5647 and T24 were used to investigate antitumor efficacy, and the result revealed that compound (15) was denoted as the most promising antitumor agent by decreasing cell viability and inducing apoptosis.…”

Section: Antitumormentioning

confidence: 99%

Some Bioactivities of Heterocyclic Compounds Containing Pyrazoline Moiety A Short Review

Ardiansah¹

2018

IJCTR

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Current research on chemistry of heterocyclic compounds is particularly focused on the development of diversity-oriented molecules containing nitrogen atom in the form of pyrazoline. Although less familiar than pyrazoles, they have shown to exhibit appreciable biological activities. This review highlights some pyrazoline compounds as promising agents for antioxidant, antitrypanosomal, antitubercular, antitumor and MAO inhibitor.

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Section: Antitumormentioning

confidence: 99%

Some Bioactivities of Heterocyclic Compounds Containing Pyrazoline Moiety A Short Review

Ardiansah¹

2018

IJCTR

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“…Furthermore, we hypothesize that intravesical injection of AdCre in the OCM platform could result in tumor formation in the bladder ( Figure 1 ); resulting in a highly valuable bladder cancer model in which new compounds and immunotherapies such as recombinant BCG (a promising immunotherapeutic approach for bladder cancer ( Begnini et al, 2015 ) could be tested. Our research group has tested the antitumoral activity of several compounds in bladder cancer cells lines using PDD approaches, including Brazilian red propolis ( Begnini et al, 2014 ) and pyrazoline derivatives ( Tessmann et al, 2017 ). A suitable animal model platform such as the OCM would further advance in vivo testing of the most promising compounds selected in these previous studies.…”

Section: Future Approachesmentioning

confidence: 99%

The Oncopig Cancer Model as a Complementary Tool for Phenotypic Drug Discovery

et al. 2017

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The screening of potential therapeutic compounds using phenotypic drug discovery (PDD) is being embraced once again by researchers and pharmaceutical companies as an approach to enhance the development of new effective therapeutics. Before the genomics and molecular biology era and the consecutive emergence of targeted-drug discovery approaches, PDD was the most common platform used for drug discovery. PDD, also known as phenotypic screening, consists of screening potential compounds in either in vitro cellular or in vivo animal models to identify compounds resulting in a desirable phenotypic change. Using this approach, the biological targets of the compounds are not taken into consideration. Suitable animal models are crucial for the continued validation and discovery of new drugs, as compounds displaying promising results in phenotypic in vitro cell-based and in vivo small animal model screenings often fail in clinical trials. Indeed, this is mainly a result of differential anatomy, physiology, metabolism, immunology, and genetics between humans and currently used pre-clinical small animal models. In contrast, pigs are more predictive of therapeutic treatment outcomes in humans than rodents. In addition, pigs provide an ideal platform to study cancer due to their similarities with humans at the anatomical, physiological, metabolic, and genetic levels. Here we provide a mini-review on the reemergence of PDD in drug development, highlighting the potential of porcine cancer models for improving pre-clinical drug discovery and testing. We also present precision medicine based genetically defined swine cancer models developed to date and their potential as biomedical models.

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“…Moreover, most novel screening approaches described in the literature do not use positive and negative clinical samples nor a single standard treatment as a reference to determine the potential predictive value of new in vitro screening techniques, making it difficult to compare the efficacy of these methodologies. Thus, our group has employed a combination of several in vitro approaches to determine the potential efficacy of novel targets, including characterization of cell death processes, cell cycle, cytotoxic mechanisms, production of reactive oxygen species, and clonogenic ability (62–66). We believe that the incorporation of multiple techniques results in a more reliable result that could be extrapolated for further in vivo tests.…”

Section: Introductionmentioning

confidence: 99%

The Melding of Drug Screening Platforms for Melanoma

et al. 2019

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The global incidence of cancer is rising rapidly and continues to be one of the leading causes of death in the world. Melanoma deserves special attention since it represents one of the fastest growing types of cancer, with advanced metastatic forms presenting high mortality rates due to the development of drug resistance. The aim of this review is to evaluate how the screening of drugs and compounds for melanoma has been performed over the last seven decades. Thus, we performed literature searches to identify melanoma drug screening methods commonly used by research groups during this timeframe. In vitro and in vivo tests are essential for the development of new drugs; however, incorporation of in silico analyses increases the possibility of finding more suitable candidates for subsequent tests. In silico techniques, such as molecular docking, represent an important and necessary first step in the screening process. However, these techniques have not been widely used by research groups to date. Our research has shown that the vast majority of research groups still perform in vitro and in vivo tests, with emphasis on the use of in vitro enzymatic tests on melanoma cell lines such as SKMEL and in vivo tests using the B16 mouse model. We believe that the union of these three approaches ( in silico, in vitro , and in vivo ) is essential for improving the discovery and development of new molecules with potential antimelanoma action. This workflow would provide greater confidence and safety for preclinical trials, which will translate to more successful clinical trials and improve the translatability of new melanoma treatments into clinical practice while minimizing the unnecessary use of laboratory animals under the principles of the 3R's.

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Antitumor potential of 1-thiocarbamoyl-3,5-diaryl-4,5-dihydro-1H-pyrazoles in human bladder cancer cells

Cited by 33 publications

References 59 publications

Some Bioactivities of Heterocyclic Compounds Containing Pyrazoline Moiety A Short Review

Some Bioactivities of Heterocyclic Compounds Containing Pyrazoline Moiety A Short Review

The Oncopig Cancer Model as a Complementary Tool for Phenotypic Drug Discovery

The Melding of Drug Screening Platforms for Melanoma

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