Matches in SemOpenAlex for { <https://semopenalex.org/work/W2521041201> ?p ?o ?g. }
- W2521041201 endingPage "6165" @default.
- W2521041201 startingPage "6149" @default.
- W2521041201 abstract "Matrix metalloproteinase-13 (MMP-13), a member of the collagenase family of enzymes, has been implicated to play a key role in the pathology of osteoarthritis. Recently, we have reported the discovery of a series of quinazoline-2-carboxamide based non-zinc-binding MMP-13 selective inhibitors, as exemplified by compound 1. We then continued our research of a novel class of zinc-binding inhibitors to obtain follow-up compounds with different physicochemical, pharmacokinetic, and biological activity profiles. In order to design selective MMP-13 inhibitors, we adopted a strategy of connecting a zinc-binding group with the quinazoline-2-carboxamide system, a unique S1' binder, by an appropriate linker. Among synthesized compounds, a triazolone inhibitor 35 exhibited excellent potency (IC50=0.071nM) and selectivity (greater than 170-fold) over other MMPs (MMP-1, 2, 3, 7, 8, 9, 10, 12, and 14) and tumor necrosis factor-α converting enzyme (TACE). In this article, the design, synthesis, and biological activity of novel zinc-binding MMP-13 inhibitors are described." @default.
- W2521041201 created "2016-09-23" @default.
- W2521041201 creator A5001043320 @default.
- W2521041201 creator A5017876385 @default.
- W2521041201 creator A5022292796 @default.
- W2521041201 creator A5031245003 @default.
- W2521041201 creator A5047180760 @default.
- W2521041201 creator A5059356350 @default.
- W2521041201 creator A5064945008 @default.
- W2521041201 creator A5081697297 @default.
- W2521041201 creator A5086300788 @default.
- W2521041201 creator A5090477990 @default.
- W2521041201 date "2016-12-01" @default.
- W2521041201 modified "2023-09-23" @default.
- W2521041201 title "Design, synthesis, and biological activity of novel, potent, and highly selective fused pyrimidine-2-carboxamide-4-one-based matrix metalloproteinase (MMP)-13 zinc-binding inhibitors" @default.
- W2521041201 cites W126120635 @default.
- W2521041201 cites W1619155498 @default.
- W2521041201 cites W1890667946 @default.
- W2521041201 cites W1896485613 @default.
- W2521041201 cites W1969179229 @default.
- W2521041201 cites W1973906784 @default.
- W2521041201 cites W1977023514 @default.
- W2521041201 cites W1979555076 @default.
- W2521041201 cites W1980942868 @default.
- W2521041201 cites W1989293290 @default.
- W2521041201 cites W1997319983 @default.
- W2521041201 cites W2012801178 @default.
- W2521041201 cites W2015375238 @default.
- W2521041201 cites W2016158798 @default.
- W2521041201 cites W2018248686 @default.
- W2521041201 cites W2026915010 @default.
- W2521041201 cites W2030738459 @default.
- W2521041201 cites W2036293026 @default.
- W2521041201 cites W2042225764 @default.
- W2521041201 cites W2042906105 @default.
- W2521041201 cites W2052650371 @default.
- W2521041201 cites W2055758035 @default.
- W2521041201 cites W2060546584 @default.
- W2521041201 cites W2063818185 @default.
- W2521041201 cites W2065943460 @default.
- W2521041201 cites W2067175433 @default.
- W2521041201 cites W2071925792 @default.
- W2521041201 cites W2074842476 @default.
- W2521041201 cites W2077641860 @default.
- W2521041201 cites W2091078620 @default.
- W2521041201 cites W2094651716 @default.
- W2521041201 cites W2106677000 @default.
- W2521041201 cites W2108028848 @default.
- W2521041201 cites W2112116103 @default.
- W2521041201 cites W2119150902 @default.
- W2521041201 cites W2119520823 @default.
- W2521041201 cites W2124456960 @default.
- W2521041201 cites W2127352232 @default.
- W2521041201 cites W2128093567 @default.
- W2521041201 cites W2132012838 @default.
- W2521041201 cites W2138960046 @default.
- W2521041201 cites W2139944425 @default.
- W2521041201 cites W2146437201 @default.
- W2521041201 cites W2150260451 @default.
- W2521041201 cites W2153833568 @default.
- W2521041201 cites W2154867920 @default.
- W2521041201 cites W2157817960 @default.
- W2521041201 cites W2157935582 @default.
- W2521041201 cites W2217918056 @default.
- W2521041201 cites W2292184199 @default.
- W2521041201 cites W2321162589 @default.
- W2521041201 cites W2331267490 @default.
- W2521041201 cites W2335685118 @default.
- W2521041201 cites W2399474893 @default.
- W2521041201 cites W2950541737 @default.
- W2521041201 cites W2952709334 @default.
- W2521041201 cites W4235790631 @default.
- W2521041201 cites W4252108671 @default.
- W2521041201 doi "https://doi.org/10.1016/j.bmc.2016.09.009" @default.
- W2521041201 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/27825552" @default.
- W2521041201 hasPublicationYear "2016" @default.
- W2521041201 type Work @default.
- W2521041201 sameAs 2521041201 @default.
- W2521041201 citedByCount "27" @default.
- W2521041201 countsByYear W25210412012017 @default.
- W2521041201 countsByYear W25210412012018 @default.
- W2521041201 countsByYear W25210412012019 @default.
- W2521041201 countsByYear W25210412012020 @default.
- W2521041201 countsByYear W25210412012021 @default.
- W2521041201 countsByYear W25210412012022 @default.
- W2521041201 countsByYear W25210412012023 @default.
- W2521041201 crossrefType "journal-article" @default.
- W2521041201 hasAuthorship W2521041201A5001043320 @default.
- W2521041201 hasAuthorship W2521041201A5017876385 @default.
- W2521041201 hasAuthorship W2521041201A5022292796 @default.
- W2521041201 hasAuthorship W2521041201A5031245003 @default.
- W2521041201 hasAuthorship W2521041201A5047180760 @default.
- W2521041201 hasAuthorship W2521041201A5059356350 @default.
- W2521041201 hasAuthorship W2521041201A5064945008 @default.
- W2521041201 hasAuthorship W2521041201A5081697297 @default.
- W2521041201 hasAuthorship W2521041201A5086300788 @default.
- W2521041201 hasAuthorship W2521041201A5090477990 @default.
- W2521041201 hasConcept C107824862 @default.