Brave New Hope for Breast Cancer Aminopyrazole derivates between rational design and clinical efficacy

Niţulescu, George Mihai; Iancu, George; Nițulescu, Georgiana; Iancu, Raluca; Bogdănici, Camelia Margareta; Vasile, D.

doi:10.37358/rc.17.4.5546

Cited by 11 publications

(10 citation statements)

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“…Each compound was tested in duplicate. Lethality was recorded after 24, 48 and 72 h, considering dead the organisms that did not move their appendages for 30 s [27]. The bioassay was performed at concentrations ranging from 3.75 to 100 µM for each compound.…”

Section: N-(3-fluorophenyl)-5-(4-(phenylsulfonyl)phenyl)-134thiadiamentioning

confidence: 99%

Synthesis and Structural Characterization of Some Potential Anti-Virulence 1,2,4-Triazoles and 1,3,4-Thiadiazoles

Bărbuceanu¹,

Olaru²,

Niţulescu³

et al. 2018

Rev. Chim.

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This paper presents a continuation of our studies in the synthesis of some 1,2,4-triazole-3-thiones and 1,3,4-thiadiazol-2-amines containing in their molecules the fluorine atom. For the synthesis of these heterocycles, the hydrazinecarbothioamides, 2-(4-(4-X-phenylsulfonyl)benzoyl)-N-(3-fluorophenyl) hydrazinecarbo-thioamides 2a-c, were obtained by treatment of some 4-(4-X-phenylsulfonyl)-benzoic acid hydrazides 1a-c with 3-fluorophenyl isothiocyanate. The new 5-(4-(4-X-phenylsulfonyl)phenyl)-4-(3-fluorophenyl)-2H-1,2,4-triazole-3(4H)-thiones 3a-c were obtained by refluxing of hydrazinecarbothioamide 2a-c with a solution natrium hidroxide and the 5-(4-(4-X-phenylsulfonyl)phenyl)-N-(3-fluorophenyl)-1,3,4-thiadiazol-2-amines 4a-c were synthesized by refluxing of hydrazinecarbothioamides 2a-c with phosphorus oxychloride. The newly synthesized compounds were characterized by IR, 1H-NMR, 13C-NMR, mass spectral data and by elemental analysis. The compounds have been tested on Daphnia magna for their toxicity assessment.

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Section: N-(3-fluorophenyl)-5-(4-(phenylsulfonyl)phenyl)-134thiadiamentioning

confidence: 99%

Synthesis and Structural Characterization of Some Potential Anti-Virulence 1,2,4-Triazoles and 1,3,4-Thiadiazoles

Bărbuceanu¹,

Olaru²,

Niţulescu³

et al. 2018

Rev. Chim.

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“…Data analysis tools such as the NCI's Developmental Therapeutics Program (DTP)'s COMPARE algorithm use these outputs on all 60 cancer cell lines to create a fingerprint profile that allows classification and can predict the mechanism of action [29,30]. The fingerprint of cellular response in the NCI-60 assay can be used to determine similar prototype compounds, and the usefulness of this data-mining approach has been demonstrated in various studies [31][32][33][34].…”

Section: Introductionmentioning

confidence: 99%

In Search of Outliers. Mining for Protein Kinase Inhibitors Based on Their Anti-Proliferative NCI-60 Cell Lines Profile

Ion

Nițulescu

2020

Molecules

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Protein kinases play a pivotal role in signal transduction, protein synthesis, cell growth and proliferation. Their deregulation represents the basis of pathogenesis for numerous diseases such as cancer and pathologies with cardiovascular, nervous and inflammatory components. Protein kinases are an important target in the pharmaceutical industry, with 48 protein kinase inhibitors (PKI) already approved on the market as treatments for different afflictions including several types of cancer. The present work focuses on facilitating the identification of new PKIs with antitumoral potential through the use of data-mining and basic statistics. The National Cancer Institute (NCI) granted access to the results of numerous previously tested compounds on 60 tumoral cell lines (NCI-60 panel). Our approach involved analyzing the NCI database to identify compounds that presented similar growth inhibition (GI) profiles to that of existing PKIs, but different from approved oncologic drugs with other mechanisms of action, using descriptive statistics and statistical outliers. Starting from 34,000 compounds present in the database, we filtered 400 which displayed selective inhibition on certain cancer cell lines similar to that of several already-approved PKIs.

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“…Deficiencies occurring during the classical stages of the fibrosis process influence the development of the patients' clinical picture [13]. Fibrosis is a natural process that is triggered during the interaction between the body and the environment, being caused by the following main factors: haemorrhage, infection [14], immune system response to allergens, foreign body reaction or neoplasm [15].…”

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confidence: 99%

Research Related to Capsular Contracture after Breast Augmentation for Cosmetic or Reconstructive Purposes

Marinescu¹,

Enescu²,

Bejinariu³

et al. 2019

Rev. Chim.

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The upward trend of patients opting for elective breast augmentation, as well as the large number of patients benefiting from alloplastic breast reconstruction, require further studies on the safety profile of these techniques. Without any doubt, the incidence of Breast Implant-Associated Anaplastic Large Cell Lymphoma (BIA-ALCL) has drawn attention to the possible unknown complications characteristic of these procedures, creating the context of further studies devoted to this issue. The present research examines the capsular contracture rate on a group of 253 patients between 2015 and 2019, also proposing a scoring system based on the integration of the main diagnostic criteria related to the capsular contracture. The results of the literature review indicate that a lower incidence of capsular contracture could be achieved by using the newest techniques in the field involving the application of chemical substances on the surface of the latest generation of silicone breast implants.

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Brave New Hope for Breast Cancer Aminopyrazole derivates between rational design and clinical efficacy

Cited by 11 publications

References 0 publications

Synthesis and Structural Characterization of Some Potential Anti-Virulence 1,2,4-Triazoles and 1,3,4-Thiadiazoles

Synthesis and Structural Characterization of Some Potential Anti-Virulence 1,2,4-Triazoles and 1,3,4-Thiadiazoles

In Search of Outliers. Mining for Protein Kinase Inhibitors Based on Their Anti-Proliferative NCI-60 Cell Lines Profile

Research Related to Capsular Contracture after Breast Augmentation for Cosmetic or Reconstructive Purposes

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