371917-81-6Relevant articles and documents
Novel 1,3-diarylpyrazole acrylamides: Synthesis, antiplatelet activity screening, and in silico evaluation studies
Baytas, Sultan Nacak,Inceler, Nazan,Ozkan, Yesim,Unlu, Serdar,Fethi Sahin
, p. 5922 - 5933 (2013)
(E)-3-[3-(pyridin-4-yl)-1-phenyl-1H-pyrazole-4-yl]acryl amides were evaluated for their antiplatelet activities. Compounds 4o and 4r were found as active derivatives showing a potent inhibitory activity on the arachidonic acid-induced aggregation, with IC50 of 20.2 and 30.3 μM, respectively. Compounds 4j, 4k, and 4u presented significant inhibitor effect on collagen-induced platelet aggregation (73.1, 82.5, and 86.7 %, respectively). All synthesized compounds demonstrated good drug-likeness and drug-score values in silico evaluations.
DNA interaction, anticancer, cytotoxicity and genotoxicity studies with potential pyrazine-bipyrazole dinuclear μ-oxo bridged Au(III) complexes
Bhatt, Bhupesh S.,Kanthecha, Darshana N.,Patel, Mohan N.,Pathak, Chandramani,Vaidya, Foram U.
, (2021/09/28)
Pyrazine-bipyrazole-based μ-oxo bridged dinuclear Au(III) complexes were synthesized and characterized by various spectrometric (1H-NMR, 13C (APT) NMR, FT-IR, Mass spectrometry) and analytical techniques (elemental analysis and condu
Discovery of pyrazole derivatives as cellular active inhibitors of histone lysine specific demethylase 5B (KDM5B/JARID1B)
Liang, Qianqian,Liu, Hong-Min,Ma, Li-Ying,Ren, Hongmei,Wu, Yang,Zhang, Kun,Zhang, Xinhui,Zhao, Bing,Zheng, Yi-Chao
, (2020/03/10)
KDM5B (also known as PLU-1 and JARID1B) is 2-oxoglutarate and Fe2+ dependent oxygenase that acts as a histone H3K4 demethylase, which is a key participant in inhibiting the expression of tumor suppressors as a drug target. Here, we present the discovery of pyrazole derivatives compound 5 by structure-based virtual screening and biochemical screening with IC50 of 9.320 μM against KDM5B, and its subsequent optimization to give 1-(4-methoxyphenyl)-N-(2-methyl-2-morpholinopropyl)-3-phenyl-1H-pyrazole-4-carboxamide (27 ab), a potent KDM5B inhibitor with IC50 of 0.0244 μM. In MKN45 cells, compound 27 ab can bind and stabilize KDM5B and induce the accumulation of H3K4me2/3, bona fide substrates of KDM5B, while keep the amount of H3K4me1, H3K9me2/3 and H3K27me2 without change. Further biological study also indicated that compound 27 ab is a potent cellular active KDM5B inhibitor that can inhibit MKN45 cell proliferation, wound healing and migration. In sum, our finding gives a novel structure for the discovery of KDM5B inhibitor and targeting KDM5B may be a new therapeutic strategy for gastric cancer treatment.
Design, synthesis and biological evaluation of novel 1,3-diarylpyrazoles as cyclooxygenase inhibitors, antiplatelet and anticancer agents
Inceler, Nazan,Ozkan, Yesim,Turan, Nilufer Nermin,Kahraman, Deniz Cansen,Cetin-Atalay, Rengul,Baytas, Sultan Nacak
supporting information, p. 795 - 811 (2018/05/31)
With the aim of achieving new compounds possessing both anti-inflammatory and antiplatelet activities, we synthesized (E)-3-[3-(pyridin-3/4-yl)-1-(phenyl/sulfonylmethylphenyl)-1H-pyrazol-4-yl]acrylamides, and evaluated their COX-1 and COX-2 inhibitory and
Synthesis and biological evaluation of novel pyrazolic chalcone derivatives as novel hepatocellular carcinoma therapeutics
Hawash, Mohammed M.A.,Kahraman, Deniz Cansen,Eren, Fikriye,Cetin Atalay, Rengul,Baytas, Sultan Nacak
, p. 12 - 26 (2017/02/23)
Despite having the second highest mortality associated with cancer, currently Sorafenib is the only FDA-approved chemotherapeutic agent available for liver cancer patients which can only improve survival for few months. In this study, various pyrazolic ch
Synthesis, antiviral, cytotoxicity and antitumor evaluations of A4 type of porphyrin derivatives
Fadda, Ahmed A.,El-Mekawy, Rasha E.,El-Shafei, Ahmed I.
, p. 753 - 768 (2015/10/29)
This manuscript describes the synthesis of a new series of porphyrin structures 4a-4m, 7, 9, 12 and 14. These structures were investigated against two types of viruses such as HIV-1 and HSV-1. Also they were screened for their antitumor activity. Among all tested compounds, it was found that compound 4b showed a high activity against HIV-1 and HSV-1 and against four different tumor cell lines. Most of the tested compounds showed a moderate degree of a potent antimicrobial activity. The structure of these compounds was confirmed on the basis of their analytical and spectral data such as UV-vis, IR, 13C NMR, 1H NMR spectroscopy and mass spectral data.
Synthesis, antiviral, cytotoxicity and antitumor evaluations of A4 type of porphyrin derivatives
Fadda, Ahmed A.,El-Mekawy, Rasha E.,El-Shafei, Ahmed I.
, p. 753 - 768 (2016/01/09)
This manuscript describes the synthesis of a new series of porphyrin structures 4a-4m, 7, 9, 12 and 14. These structures were investigated against two types of viruses such as HIV-1 and HSV-1. Also they were screened for their antitumor activity. Among all tested compounds, it was found that compound 4b showed a high activity against HIV-1 and HSV-1 and against four different tumor cell lines. Most of the tested compounds showed a moderate degree of a potent antimicrobial activity. The structure of these compounds was confirmed on the basis of their analytical and spectral data such as UV-vis, IR, 13C NMR, 1H NMR spectroscopy and mass spectral data.
Synthesis, cytotoxicity, and molecular properties prediction of novel 1,3-diarylpyrazole derivatives
Baytas, Sultan Nacak,Inceler, Nazan,Yilmaz, Akin
, p. 4893 - 4908 (2013/09/23)
A novel combinatorial library of ester and amide derivatives of 1,3-diarylpyrazoles was designed and synthesized. Anticancer activities of these compounds were assessed against MCF7, MDA-MB-231, HeLa, Raji, and HL60 human cancer cells by MTT assay. Out of
Synthesis, characterization, and biological screening of some novel thiazolidin-4-One and α-aminophosphonate derivatives
Badadhe,Chavan,Ghotekar,Mandhane,Joshi,Gill
, p. 2021 - 2032 (2011/12/03)
Synthesis of some new functionalized thiazolidin-4-ones and α-amino phosphonate derivatives has been reported. The imines were synthesized from the reaction of various substituted anilines with 1-phenyl-3-(pyridine-4-yl)-1H- pyrazole-4-carbaldehyde in eth
