ArticleBioorganic & medicinal chemistry letters2012
Synthesis and biological activity of 2-aminothiazoles as novel inhibitors of PGE2 production in cells.
Article in Bioorganic & medicinal chemistry letters, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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Who cites it
5 citing papers in PubMed.
- Exploring novel thiazolo[5,4-f]quinoline-based scaffolds as promising antimicrobial agents through synthesis and molecular insights.Scientific reports · 2025Article
- Vinyl azides in organic synthesis: an overview.RSC advances · 2023Review
- Article
- Targeting mPGES-1 by a Combinatorial Approach: Identification of the Aminobenzothiazole Scaffold to Suppress PGEACS medicinal chemistry letters · 2020Article
- Synthesis and biological activity of aminophthalazines and aminopyridazines as novel inhibitors of PGE2 production in cells.Bioorganic & medicinal chemistry letters · 2013Article
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Authors and funding
8 authors.
Funding
Abstract
This Letter presents the synthesis and biological evaluation of a collection of 2-aminothiazoles as a novel class of compounds with the capability to reduce the production of PGE(2) in HCA-7 human adenocarcinoma cells. A total of 36 analogs were synthesized and assayed for PGE(2) reduction, and those with potent cellular activity were counter screened for inhibitory activity against COX-2 in a cell free assay. In general, analogs bearing a 4-phenoxyphenyl substituent in the R(2) position were highly active in cells while maintaining negligible COX-2 inhibition. Specifically, compound 5l (R(1)=Me, R(2)=4-OPh-Ph, R(3)=CH(OH)Me) exhibited the most potent cellular PGE(2) reducing activity of the entire series (EC(50)=90 nM) with an IC(50) value for COX-2 inhibition of >5 μM in vitro. Furthermore, the anti-tumor activity of analog 1a was analyzed in xenograft mouse models exhibiting promising anti-cancer activity.
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Registered trials
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