Matches in SemOpenAlex for { <https://semopenalex.org/work/W2316753968> ?p ?o ?g. }
- W2316753968 endingPage "5394" @default.
- W2316753968 startingPage "5382" @default.
- W2316753968 abstract "Starting from our in-house library of pyrazolo[3,4-d]pyrimidines, a cross-docking simulation was conducted on Bcr-Abl T315I mutant. Among the selected compounds (2a–e), the 4-bromo derivative 2b showed the best activity against the Bcr-Abl T315I mutant. Deeper computational studies highlighted the importance of the bromine atom in the para position of the N1 side chain phenyl ring for the interaction with the T315I mutant. A series of 4-bromo derivatives was thus synthesized and biologically evaluated. Compound 2j showed a good balance of different ADME properties, high activity in cell-free assays, and a submicromolar potency against T315I Bcr-Abl expressing cells. In addition, it was converted into a water-soluble formulation by liposome encapsulation, preserving a good activity on leukemic T315I cells and avoiding the use of DMSO as solubilizing agent. In vivo studies on mice inoculated with 32D-T315I cells and treated with 2j showed a more than 50% reduction in tumor volumes." @default.
- W2316753968 created "2016-06-24" @default.
- W2316753968 creator A5001780639 @default.
- W2316753968 creator A5006417481 @default.
- W2316753968 creator A5008783082 @default.
- W2316753968 creator A5008959072 @default.
- W2316753968 creator A5010109904 @default.
- W2316753968 creator A5016372629 @default.
- W2316753968 creator A5019708105 @default.
- W2316753968 creator A5046402166 @default.
- W2316753968 creator A5046778355 @default.
- W2316753968 creator A5056135019 @default.
- W2316753968 creator A5056536140 @default.
- W2316753968 creator A5068650467 @default.
- W2316753968 creator A5068941229 @default.
- W2316753968 creator A5090204935 @default.
- W2316753968 creator A5090835353 @default.
- W2316753968 creator A5091202892 @default.
- W2316753968 date "2013-06-20" @default.
- W2316753968 modified "2023-10-16" @default.
- W2316753968 title "Design, Synthesis, and Biological Evaluation of Pyrazolo[3,4-<i>d</i>]pyrimidines Active in Vivo on the Bcr-Abl T315I Mutant" @default.
- W2316753968 cites W1545266804 @default.
- W2316753968 cites W1975196156 @default.
- W2316753968 cites W1984160018 @default.
- W2316753968 cites W1985510130 @default.
- W2316753968 cites W1990161102 @default.
- W2316753968 cites W1993201051 @default.
- W2316753968 cites W1993675254 @default.
- W2316753968 cites W2024951966 @default.
- W2316753968 cites W2028841370 @default.
- W2316753968 cites W2034948450 @default.
- W2316753968 cites W2035019841 @default.
- W2316753968 cites W2036026697 @default.
- W2316753968 cites W2043668344 @default.
- W2316753968 cites W2052030759 @default.
- W2316753968 cites W2054251966 @default.
- W2316753968 cites W2056516302 @default.
- W2316753968 cites W2063350668 @default.
- W2316753968 cites W2063779505 @default.
- W2316753968 cites W2066998725 @default.
- W2316753968 cites W2071504476 @default.
- W2316753968 cites W2073101936 @default.
- W2316753968 cites W2076271269 @default.
- W2316753968 cites W2077384736 @default.
- W2316753968 cites W2090004346 @default.
- W2316753968 cites W2092606584 @default.
- W2316753968 cites W2093429872 @default.
- W2316753968 cites W2095745765 @default.
- W2316753968 cites W2096861064 @default.
- W2316753968 cites W2097177625 @default.
- W2316753968 cites W2099634712 @default.
- W2316753968 cites W2103445331 @default.
- W2316753968 cites W2105763112 @default.
- W2316753968 cites W2110648386 @default.
- W2316753968 cites W2132348188 @default.
- W2316753968 cites W2136065656 @default.
- W2316753968 cites W2148763134 @default.
- W2316753968 cites W2150148922 @default.
- W2316753968 cites W2154437955 @default.
- W2316753968 cites W2170372518 @default.
- W2316753968 cites W2170527434 @default.
- W2316753968 cites W2334727267 @default.
- W2316753968 cites W2950018626 @default.
- W2316753968 doi "https://doi.org/10.1021/jm400233w" @default.
- W2316753968 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/23746084" @default.
- W2316753968 hasPublicationYear "2013" @default.
- W2316753968 type Work @default.
- W2316753968 sameAs 2316753968 @default.
- W2316753968 citedByCount "38" @default.
- W2316753968 countsByYear W23167539682014 @default.
- W2316753968 countsByYear W23167539682015 @default.
- W2316753968 countsByYear W23167539682016 @default.
- W2316753968 countsByYear W23167539682017 @default.
- W2316753968 countsByYear W23167539682018 @default.
- W2316753968 countsByYear W23167539682019 @default.
- W2316753968 countsByYear W23167539682020 @default.
- W2316753968 countsByYear W23167539682021 @default.
- W2316753968 countsByYear W23167539682022 @default.
- W2316753968 countsByYear W23167539682023 @default.
- W2316753968 crossrefType "journal-article" @default.
- W2316753968 hasAuthorship W2316753968A5001780639 @default.
- W2316753968 hasAuthorship W2316753968A5006417481 @default.
- W2316753968 hasAuthorship W2316753968A5008783082 @default.
- W2316753968 hasAuthorship W2316753968A5008959072 @default.
- W2316753968 hasAuthorship W2316753968A5010109904 @default.
- W2316753968 hasAuthorship W2316753968A5016372629 @default.
- W2316753968 hasAuthorship W2316753968A5019708105 @default.
- W2316753968 hasAuthorship W2316753968A5046402166 @default.
- W2316753968 hasAuthorship W2316753968A5046778355 @default.
- W2316753968 hasAuthorship W2316753968A5056135019 @default.
- W2316753968 hasAuthorship W2316753968A5056536140 @default.
- W2316753968 hasAuthorship W2316753968A5068650467 @default.
- W2316753968 hasAuthorship W2316753968A5068941229 @default.
- W2316753968 hasAuthorship W2316753968A5090204935 @default.
- W2316753968 hasAuthorship W2316753968A5090835353 @default.
- W2316753968 hasAuthorship W2316753968A5091202892 @default.
- W2316753968 hasConcept C104317684 @default.
- W2316753968 hasConcept C143065580 @default.