5071-61-4Relevant academic research and scientific papers
Pyrazoleamide derivative and synthesis method and application
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Paragraph 0048; 0073-0074, (2022/01/10)
The present invention discloses a pyrazoleamide derivative and a synthetic method and application as an androgen receptor antagonist and the preparation of anti-prostate cancer drugs. The present invention provides a method of synthesizing a pentabasole r
Discovery of Membrane-Bound Pyrophosphatase Inhibitors Derived from an Isoxazole Fragment
Johansson, Niklas G.,Turku, Ainoleena,Vidilaseris, Keni,Dreano, Lo?c,Khattab, Ayman,Ayuso Pérez, Daniel,Wilkinson, Aaron,Zhang, Yuezhou,Tamminen, Matti,Grazhdankin, Evgeni,Kiriazis, Alexandros,Fishwick, Colin W. G.,Meri, Seppo,Yli-Kauhaluoma, Jari,Goldman, Adrian,Boije Af Genn?s, Gustav,Xhaard, Henri
supporting information, p. 605 - 610 (2020/03/10)
Membrane-bound pyrophosphatases (mPPases) regulate energy homeostasis in pathogenic protozoan parasites and lack human homologues, which makes them promising targets in e.g. malaria. Yet only few nonphosphorus inhibitors have been reported so far. Here, w
Pyrazole amide derivatives as well as preparation method and application thereof
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Paragraph 0140; 0147-0150, (2019/05/16)
The invention relates to pyrazole derivatives represented by a general formula I shown in the description, or a stereoisomer and tautomer of the pyrazole derivatives, a preparation method of the pyrazole derivatives, and an application of the of the pyraz
Fragment-based lead generation of 5-phenyl-1H-pyrazole-3-carboxamide derivatives as leads for potent factor xia inhibitors
Wei, Qunchao,Zheng, Zhichao,Zhang, Shijun,Zheng, Xuemin,Meng, Fancui,Yuan, Jing,Xu, Yongnan,Huang, Changjiang
, (2018/09/26)
FXIa is suggested as a major target for anticoagulant drug discovery because of reduced risk of bleeding. In this paper, we defined 5-phenyl-1H-pyrazole-3-carboxylic acid derivatives as privileged fragments for FXIa inhibitors' lead discovery. After repla
FIVE-MEMBERED HETEROCYCLIC AMIDES WNT PATHWAY INHIBITOR
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, (2018/10/19)
The present invention discloses a five-membered heterocyclic amide WNT pathway inhibitor, which belongs to a compound that regulates the activity of a Wnt signaling pathway, and provides a method for preparing such a compound, and the use of such a compound in preparing a medicament that antagonizes the Wnt signaling pathway. The five-membered heterocyclic amide WNT pathway inhibitor provided by the invention has a remarkable anti-tumor activity based on a target-based rational drug design of, and can be used for the development of a new generation of Wnt pathway inhibitors, and has a great clinical application value and considerable market potential.
PAR2 RECEPTOR ANTAGONISTS
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Page/Page column 51, (2014/02/16)
Compounds of formula (I) or pharmaceutically acceptable salts, solvates or hydrates thereof wherein P, Q, X, Y, R1, R2, R3, R10, R11, and R12 are as defined in the claims, and the use those compounds in medicine.
RECEPTOR ANTAGONISTS
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Page/Page column 36, (2014/02/16)
N-(4-carbamimidoylphenyl)-amide derivatives having utility in therapy as PAR2 receptor antagonists.
Pyrazole derivatives as potent inhibitors of c-Jun N-terminal kinase: Synthesis and SAR studies
Doma, Anuradha,Kulkarni, Ravindra,Palakodety, Radhakrishna,Sastry, G. Narahari,Sridhara, Janardhan,Garlapati, Achaiah
, p. 6209 - 6219 (2014/12/11)
Mitogen activated protein kinases including c-Jun N-terminal kinase play an indispensable role in inflammatory diseases. Investigation of reported JNK-1 inhibitors indicated that diverse heterocyclic compounds bearing an amide group rendered potent JNK-1 inhibitory activity which prompted us to synthesize new JNK-1 inhibitors containing a pyrazole heterocyclic group. A DABCO mediated 1,3-dipolar cycloaddition reaction in neat resulted in pyrazole carboxylic acid which was converted to desired amides. Upon confirmation of the structures, all the compounds were screened for JNK-1 inhibitory activity and in vivo anti-inflammatory activity. Several synthesized analogues have exhibited JNK-1 inhibitory activity less than 10 μM, in particular compounds 9c, 10a and 10d were found to be potent among all the compounds.
Synthesis and anticancer activity of heteroaromatic linked 4β-amido podophyllotoxins as apoptotic inducing agents
Kamal, Ahmed,Tamboli, Jaki R.,Vishnuvardhan,Adil,Nayak, V. Lakshma,Ramakrishna
, p. 273 - 280 (2013/02/25)
A series of different heteroaromatic linked 4β-amidopodophyllotoxin conjugates (16a-i, 17a-i and 18a-d) were synthesized and evaluated for anticancer activity against five human cancer cell lines. Among the series, one of the compound 17g showed significant antiproliferative activity in A549 (lung cancer) cell line. Flow cytometric analysis showed that 17g arrested the cell cycle in the G2/M phase leading to caspase-3 dependent apoptotic cell death. Further, Hoechst 33258 staining and DNA fragmentation assay also suggests that 17g induces cell death by apoptosis.
Pyrazole-3/5-carboxylic acids from 3/5-trifluoromethyl NH-pyrazoles
Ermolenko, Mikhail S.,Guillou, Sandrine,Janin, Yves L.
, p. 257 - 263 (2013/01/15)
We report here the transformation of 3/5-trifluoromethylpyrazoles derivative into the corresponding NH-pyrazole-3/5-carboxylic acids. Moreover, from 4- or 5-iodinated-3/5-trifluoromethylpyrazoles building blocks and the use of Suzuki-Miyaura or Negishi reactions followed by the trifluoromethyl hydrolysis, we illustrate short and original accesses to many series of NH-pyrazole-3/5-carboxylic acids otherwise difficult to prepare.
