Literature DB >> 16380252

5-Heteroatom-substituted pyrazoles as canine COX-2 inhibitors: Part 2. Structure-activity relationship studies of 5-alkylethers and 5-thioethers.

Subas M Sakya1, Hengmiao Cheng, Kristin M Lundy Demello, Andrei Shavnya, Martha L Minich, Bryson Rast, Jason Dutra, Chao Li, Robert J Rafka, David A Koss, Jin Li, Burton H Jaynes, Carl B Ziegler, Donald W Mann, Carol F Petras, Scott B Seibel, Annette M Silvia, David M George, Anne Hickman, Michelle L Haven, Michael P Lynch.   

Abstract

Structure-activity relationship (SAR) studies of novel 2-[3-trifluoromethyl-5-alkyl(thio)ether pyrazo-1-yl]-5-methanesulfonyl pyridine derivatives for canine COX enzymes are described. The 4-cyano-5-alkyl ethers were found to have excellent potency and selectivity, whereas the 5-thioethers were potent but less selective than the ether analogs in a canine whole blood (CWB) COX-2 assay.

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Year:  2005        PMID: 16380252     DOI: 10.1016/j.bmcl.2005.11.110

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

Review 1.  Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.

Authors:  Khalid Karrouchi; Smaail Radi; Youssef Ramli; Jamal Taoufik; Yahia N Mabkhot; Faiz A Al-Aizari; M'hammed Ansar
Journal:  Molecules       Date:  2018-01-12       Impact factor: 4.411

2.  Microwave-assisted one pot three-component synthesis of some novel pyrazole scaffolds as potent anticancer agents.

Authors:  Sobhi M Gomha; Mastoura M Edrees; Rasha A M Faty; Zeinab A Muhammad; Yahia N Mabkhot
Journal:  Chem Cent J       Date:  2017-05-08       Impact factor: 4.215

3.  PCW-1001, a Novel Pyrazole Derivative, Exerts Antitumor and Radio-Sensitizing Activities in Breast Cancer.

Authors:  Minsung Kang; Navin Pandit; Ah-Young Kim; Suk Joon Cho; Young-Ju Kwon; Jiyeon Ahn; Kyu Myung Lee; Sangwook Wu; Jeong Su Oh; Kwan-Young Jung; Jae-Sung Kim
Journal:  Front Oncol       Date:  2022-03-29       Impact factor: 6.244

  3 in total

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