5767-35-1Relevant academic research and scientific papers
Novel pyrimidine derivatives as potential anticancer agents: Synthesis, biological evaluation and molecular docking study
Tylińska, Beata,Wiatrak, Benita,Czy?nikowska, ?aneta,Cie?la-Niechwiadowicz, Aneta,G?barowska, El?bieta,Janicka-K?os, Anna
, (2021)
In the present paper, new pyrimidine derivatives were designed, synthesized and analyzed in terms of their anticancer properties. The tested compounds were evaluated in vitro for their antitu-mor activity. The cytotoxic effect on normal human dermal fibroblasts (NHDF) was also determined. According to the results, all the tested compounds exhibited inhibitory activity on the proliferation of all lines of cancer cells (colon adenocarcinoma (LoVo), resistant colon adenocarcinoma (LoVo/DX), breast cancer (MCF-7), lung cancer (A549), cervical cancer (HeLa), human leukemic lymphoblasts (CCRF-CEM) and human monocytic (THP-1)). In particular, their feature stronger influence on the activity of P-glycoprotein of cell cultures resistant to doxorubicin than doxorubicin. Tested compounds have more lipophilic character than doxorubicin, which determines their affinity for the molecular target and passive transport through biological membranes. Moreover, the inhibitory potential against topoisomerase II and DNA intercalating properties of synthesized compounds were analyzed via molecular docking.
Antioxidant and antimicrobial properties of nickel(II), cobalt(III), and zinc(II) complexes of a Schiff base ligand
Hasi, Qi-Meige,Fan, Yan,Feng, Xiao-Xia,Yao, Xiao-Qiang,Liu, Jia-Cheng
, p. 685 - 692 (2016)
A series of mononuclear Ni(II), Co(III), and Zn(II) complexes based on a Schiff base ligand, 4-chloro-6-[2-(pyrazin-2-ylmethylene)hydrazinyl]pyrimidine (HL), have been synthesized and characterized by physicochemical and spectroscopic methods. The complexes were found to have superior radical scavenging potency against DPPH, superoxide anion, hydroxyl, and ABTS radicals than free HL. The antibacterial effects of the complexes against Gram-positive and Gram-negative bacteria were also higher than that of free HL.
In silico and in vitro Antitubercular Studies for Nitrogen Rich Hybrids of homopiperazine-pyrimidine-Pyrazole Adducts
Marvaniya, Vanita,Pansuriya, Vrajlal,Patel, Popatbhai,Patel, Shivani,Vavaiya, Bhavinkumar
, p. 562 - 568 (2022/02/22)
Novel homopiperazine-pyrimidine-pyrazole hybrids (3a-j) were synthesized using ethyl 2-cyanoacetate and 4,6-dichloropyrimidine as starting materials by a multi-step process to afford ethyl 5-amino-1-(6-chloropyrimidin-4-yl)-1H-pyrazole-4-carboxylate in good yields using polar protic media. The intermediate 1, in two steps, chloroamine condensation followed by acid amine coupling, furnished the title compounds ethyl 5-amino-1-(6-(4-substituted aryl-1,4-diazepan-1-yl)pyrimidin-4-yl)-1H-pyrazole-4-carboxylate (3a-j). The synthesized compounds were docked in the crystal structure of Mycobacterium tuberculosis (PDB ID: 4TRO) to get insights into structural requirements for antitubercular activity. In vitro antitubercular activity against M. tuberculosis H37Rv strains showed that compounds 3a, 3d, 3e and 3g were found to be the most potent (Docking score: > -21; MIC = 1.6 μg/mL) among the synthesized molecules. All the synthesized compounds showed acceptable drug-like properties which make them suitable for further lead modification using in silico design approaches.
ErbB RECEPTOR INHIBITORS AS ANTI-TUMOR AGENTS
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Page/Page column 132; 133, (2021/09/17)
Provided herein are novel compounds as inhibitors of type I receptor tyrosine kinases, the pharmaceutical compositions comprising one or more of the compounds and salts thereof as an active ingredient, and the use of the compounds and salts thereof in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals and especially in humans.
GPR52 MODULATOR COMPOUNDS
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Paragraph 73-74, (2021/05/15)
The disclosures herein relate to novel compounds of Formula (1): (1) and salts thereof, wherein R1, Q, X, Y and Z are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with GPR52 receptors.
QUINAZOLINE DERIVATIVES AS ANTITUMOR AGENTS
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Page/Page column 95-96, (2020/04/25)
The present application relates to novel quinazoline compounds as inhibitors of type I receptor tyrosine kinases, the pharmaceutical compositions comprising one or more of the compounds and salts thereof as an active ingredient, and the use of the compounds and salts thereof in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals and especially in humans.
Pyrimidine hydrazone derivative and preparation method and application thereof
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Paragraph 0036-0037; 0044-0046, (2020/11/23)
The invention relates to pyrimidine hydrazone derivatives as shown in a chemical structural formula I or II, pharmaceutically acceptable salts and pharmaceutical compositions thereof, and an application of the pyrimidine hydrazone derivatives and the pharmaceutically acceptable salts and the pharmaceutical compositions in preparation of influenza virus neuraminidase inhibitors, wherein X is selected from: fluorine, chlorine, bromine, hydroxyl, dihydroxy, 2-hydroxy-3-methoxy, 2-hydroxy-4-methoxy, 2-hydroxy-5-C1-C2 alkoxy, 2-hydroxy-6-C1-C2 alkoxy, 3-hydroxy-2-C1-C2 alkoxy, 3-hydroxy-4-C1-C2 alkoxy, 3-hydroxy-5-methyl C1-C2 alkoxy , 3-hydroxy-6-C1-C2 alkoxy, 4-hydroxy-2-C1-C2 alkoxy, 4-hydroxy-3-C1-C2 alkoxy, 4-hydroxy-3, 5-diC1-C2 alkoxy, trihydroxy or 4-hydroxy-3,5-dimethyl; and Y is selected from: fluorine, chlorine, bromine, acetamido, hydroxyl or methoxy.
Design, synthesis, and anticancer evaluation of acetamide and hydrazine analogues of pyrimidine
Chashoo, Gousia,Khazir, Jabeena,Maqbool, Tariq,Mir, Bilal Ahmad,Pilcher, Lynne,Riley, Darren
, (2020/02/05)
A library of acetamide and hydrazine analogues were generated on the pyrimidine ring through a multistep reaction starting from 5-nitro-pyrimidine-4,6-diol and pyrimidine-4,6-diol, respectively. The synthesized analogues were screened for in vitro cytotoxic activity against various human cancer cell lines like HCT-1 and HT-15 (colon), MCF-7(breast), PC-3 (prostrate), SF268 (CNS) using MTT method. From the bioassay results, it was observed that even though many of the synthesized derivatives exhibited a good potency against various screened cancer cell lines, compound 14a from the acetamide series was found to show potent anticancer activity on all the tested cancer cell lines with IC50 value of 0.36μM on CNS cell line and 1.6μM on HT-21 cell line, and compound 19xxi from hydrazine series of pyrimidine showed potent activity against three tested cancer cell lines with IC50 value of 0.76μM on HT-29 cell line, 2.6μM on HCT-15, and 3.2μM on MCF-7 cell line.
New crystal forms of dihydropyrazolone compound and preparation method of new crystal form
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Paragraph 0082-0084; 0089; 0090, (2020/11/05)
The invention relates to new crystal forms of a dihydropyrazolone compound and a preparation method of the new crystal form. Specifically, the invention relates to a crystal form A and a crystal formB of 1-(6-(2-oxa-8-azaspiro [4.5] decane-8-yl) pyrimidine-4-yl)-4-(1H-1, 2, 3-triazole-1-yl)-1, 2-dihydro-1H-pyrazole-3-sodium phenolate. The preparation method comprises the following steps: preparing 2-(6-(2-oxa-8-azaspiro [4.5] decane-8-yl) pyrimidine-4-yl)-4-(1H-1, 2, 3-triazole-1-yl)-1, 2-dihydro-3H-pyrazole-3-one into a sodium salt in an organic solvent, and crystallizing, thereby obtainingthe product. The new crystal forms of the dihydropyrazolone compound can be used to prevent and/or treat diseases associated with PHD activity.
New crystal forms of PHD inhibitor and preparation method thereof
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Paragraph 0077-0079; 0084; 0085, (2020/11/05)
The invention relates to new crystal forms of a PHD inhibitor and a preparation method of the new crystal forms. Specifically, the invention relates to a crystal form A and a crystal form B of 1-(6-(7-oxa-2-azaspiro [3.5] non-2-yl) pyrimidine-4-yl)-4-(1H-1, 2, 3-triazole-1-yl)-1, 2-dihydro-3H-pyrazole-3-sodium phenolate. The preparation method comprises the following steps: preparing 2-(6-(7-oxa-2-azaspiro [3.5] non-2-yl) pyrimidine-4-yl)-4-(1H-1, 2, 3-triazole-1-yl)-1, 2-dihydro-3H-pyrazole-3-one into a sodium salt in an organic solvent, and crystallizing, thereby obtaining the product. It can be used to prevent and/or treat diseases associated with PHD activity.
