29338-66-7Relevant academic research and scientific papers
Synergistic effect of pyrazoles derivatives and doxorubicin in claudin-low breast cancer subtype
Saueressig, Silvia,Tessmann, Josiane,Mastelari, Rosiane,da Silva, Liziane Pereira,Buss, Julieti,Segatto, Natalia Vieira,Begnini, Karine Rech,Pacheco, Bruna,de Pereira, Cláudio Martin Pereira,Collares, Tiago,Seixas, Fabiana K?mmling
, p. 390 - 398 (2018)
Background Breast cancer is a global public health problem. For some subtypes, such as Claudin-low, the prognosis is poorer and the treatment is still a challenge. Pyrazoles are an important class of heterocyclic compounds and are promising anticancer age
Microwave Assisted Synthesis of Thiocarbamoylpyrazoles and Application as an Alternative Latent Fingermark Developers
Camacho, Jeanifer T.,Carre?o, Neftalí L. V.,Mariotti, Kristiane C.,Pereira, Claudio M. P.,Pizzuti, Lucas,Poletti, Taís,Venzke, Dalila,da Rosa, Bruno N.,de Lima, Nathalia P. K.,dos Santos, Marco A. Z.
, p. 1327 - 1331 (2020/10/14)
Fingerprints are unique to each individual, contributing to human identification in forensic cases. The powder technique being widely used is considered one of the most important in latent fingermarks analysis. In this sense, the present work aimed to syn
Some thiocarbamoyl based novel anticathepsin agents
Kaur, Ravinder,Raghav, Neera
supporting information, (2020/09/16)
Cathepsins have emerged as important targets in various tissues degenerative disorders due to their involvement in degradation of extracellular matrices and endogenous protein turnover. Elevated cathepsins levels vis-à-vis decreased concentration of endogenous inhibitors has been reported at different diseased sites. The design and synthesis of specific potential anti-cathepsin agents is therefore of great significance. Most of potential anti-cathepsin agents developed have peptide based structures with an active warhead. Due to oral instability and immunogenic problems related to peptidyl inhibitors drift the synthesis and evaluation of non-peptide cathepsin inhibitors in last two decades. The present work provides a detailed structure activity relationship for developing potential non-peptide anticathepsin agents based on in-vitro inhibition studies of a library of synthesized thiocarbamoyl- non-peptide inhibitors.
Discovery of new fluorescent thiazole–pyrazoline derivatives as autophagy inducers by inhibiting mTOR activity in A549 human lung cancer cells
Chen, Yuan,Gao, DongFang,Kong, Feng,Lin, YuXing,Lin, ZhaoMin,Miao, JunYing,Wang, Peng,Wang, ZhaoYang,Zhang, Lu,Zhang, Ming,Zhao, BaoXiang,Zhou, XueWen
, (2020/07/25)
A series of fluorescent thiazole–pyrazoline derivatives was synthesized and their structures were characterized by 1H NMR, 13C NMR, and HRMS. Biological evaluation demonstrated that these compounds could effectively inhibit the growt
Antitumor potential of 1-thiocarbamoyl-3,5-diaryl-4,5-dihydro-1H-pyrazoles in human bladder cancer cells
Tessmann, Josiane Weber,Buss, Julieti,Begnini, Karine Rech,Berneira, Lucas Moraes,Paula, Favero Reisdorfer,de Pereira, Claudio Martin Pereira,Collares, Tiago,Seixas, Fabiana K?mmling
, p. 37 - 46 (2017/07/27)
Bladder cancer is a genitourinary malignant disease common worldwide. Current chemotherapy is often limited mainly due to toxicity and drug resistance. Thus, there is a continued need to discover new therapies. Recently evidences shows that pyrazoline der
Synergistic antifungal effect of cyclized chalcone derivatives and fluconazole against Candida albicans
Ahmad, Aijaz,Wani, Mohmmad Younus,Patel, Mrudula,Sobral, Abilio J.F.N.,Duse, Adriano G.,Aqlan, Faisal Mohammed,Al-Bogami, Abdullah Saad
, p. 2195 - 2207 (2017/12/26)
The occurrence of invasive fungal diseases, particularly in immunocompromised patients, is life-threatening and increases the economic burden. The rising problem of multi-drug resistance is becoming a major concern for clinicians. In addition, a repertoire of antifungal agents is far less in number than antibacterial drugs. To combat these problems, combination therapy has gained a lot of interest. We previously reported the synergistic interaction of some mono- and bis-dihydropyrimidinone and thione derivatives with fluconazole and amphotericin B for combination antifungal therapy. In this study we used the same approach and synthesized different azole and non-azole derivatives of mono-(M) and bis-(B) chalcones and evaluated their antifungal activity profile alone and in combination with the most commonly used antifungal drug-fluconazole (FLC)-against seven FLC susceptible and three FLC resistant clinically isolated Candida albicans strains. Based on the minimum inhibitory concentration results, the bis-derivatives showed lower MIC values compared to their mono-analogues. Both fractional inhibitory concentration index and isobologram results revealed mostly synergistic, additive or indifferent interactions between the tested compounds and FLC against different Candida isolates. None of the tested compounds showed any effect on energy dependent R6G efflux, revealing that they do not reverse the mechanism of drug efflux. However, surprisingly, these compounds profoundly decreased ergosterol biosynthesis and showed down regulation of ERG11 gene expression, which is the possible mechanism of reversal of azole drug resistance by these compounds. These results provide a platform for further research to develop pyrimidinone/thione ring containing compounds as promising new antifungal agents, which could be used in antifungal combination therapy.
Experimental and quantum chemical studies on the corrosion inhibition effect of synthesized pyrazole derivatives on mild steel in hydrochloric acid
Ouici,Benali,Guendouzi
, p. 7085 - 7109 (2016/08/25)
Two heterocyclic compounds of the pyrazole family were synthesized by cyclocondensation reaction of chalcone derivatives with thiosemicarbazide. The structures of the synthesized pyrazoles, namely, 3,5-diphenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide (DP
Structure-guided discovery of 1,3,5-triazine-pyrazole conjugates as antibacterial and antibiofilm agent against pathogens causing human diseases with favorable metabolic fate
Singh, Babita,Bhat, Hans Raj,Kumawat, Mukesh Kumar,Singh, Udaya Pratap
, p. 3321 - 3325 (2014/07/22)
Impressed by the exceptional antibacterial activity exhibited by our earlier designed molecules originating from 1,3,5-triazine, the present study was undertaken to synthesize a novel series of 1,3,5-triazine-pyrazole conjugates to bring diversity around the core skeleton. The target analogues showed potent antibacterial activity against tested Gram-positive and Gram-negative microorganisms. The toxicity and metabolic site prediction studies were also held out to set an effective lead candidate for the future antibacterial drug discovery initiatives.
Design, synthesis and biological evaluation of pyrazolyl-thiazolinone derivatives as potential EGFR and HER-2 kinase inhibitors
Qiu, Ke-Ming,Wang, Hai-Hong,Wang, Li-Ming,Luo, Yin,Yang, Xian-Hui,Wang, Xiao-Ming,Zhu, Hai-Liang
experimental part, p. 2010 - 2018 (2012/05/04)
A series of pyrazolyl-thiazolinone derivatives (E1-E36) have been designed and synthesized and their biological activities were also evaluated as potential EGFR and HER-2 kinase inhibitors. Thirty-four of the 36 compounds were reported for the first time. Among them, compound 2-(5-(4-bromophenyl)-3-p-tolyl-4,5- dihydro-1H-pyrazol-1-yl)thiazol-4(5H)-one (E28) displayed the most potent inhibitory activity (IC50 = 0.24 μM for EGFR and IC50 = 1.07 μM for HER-2). Antiproliferative assay results indicated that compound E28 owned high antiproliferative activity against MCF-7, B16-F10 and HCT-116 in vitro, with IC50 value of 0.30, 0.54, and 0.70 μM, respectively. Docking simulation was further performed to position compound E28 into the EGFR active site to determine the probable binding model. Based on the preliminary results, compound E28 with potent inhibitory activity in tumor growth would be a potential anticancer agent.
Synthesis and selective inhibitory activity against human COX-1 of novel 1-(4-substituted-thiazol-2-yl)-3,5-di(hetero)aryl-pyrazoline derivatives
Carradori, Simone,Secci, Daniela,Bolasco, Adriana,De Monte, Celeste,Yá?ez, Matilde
, p. 973 - 979 (2013/02/23)
Novel 1-(4-ethyl carboxylate-thiazol-2-yl)-3,5-di(hetero)aryl-2-pyrazoline derivatives were obtained by reacting 3,5-di(hetero)aryl-1-thiocarbamoyl-2- pyrazolines with the ethyl ester of α-bromo-pyruvic acid. The synthesized compounds were confirmed by spectroscopic data and assayed to evaluate their in vitro ability to inhibit both isoforms of human cyclooxygenase (hCOX). Some derivatives (compounds 5, 6, 13, 16, and 17) displayed promising selectivity against hCOX-1 in the micromolar range and were shown to have a selectivity index similar or better than the reference drugs (indometacin, diclofenac). The introduction of a phenyl or a 4-F-phenyl ring on the C5 associated with a 4-substituted phenyl or a heteroaryl group on the C3 of (4-substituted-thiazol- 2-yl)pyrazoline derivatives improved the activity against hCOX-1. Thanks to these preliminary results it could be possible to extend our knowledge of the pharmacophoric requirements for the discovery of new pyrazoline-based hCOX-1 inhibitors. Novel 1-(4-ethyl carboxylate-thiazol-2-yl)-3,5-di(hetero)aryl-2- pyrazoline derivatives were obtained by reacting 3,5-di(hetero)aryl-1- thiocarbamoyl-2-pyrazolines with the ethyl ester of α-bromo-pyruvic acid. Some derivatives displayed promising selectivity against human cyclooxygenase 1 (hCOX-1) in the micromolar range, with a selectivity index similar or better than the reference drugs, indometacin and diclofenac. Copyright
