Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation

Search Page

Filters

My NCBI Filters

Text availability

Article attribute

Article type

Publication date

Search Results

80 results

Filters applied: . Clear all
Results are displayed in a computed author sort order. The Results By Year timeline is not available.
Page 1
Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant.
Huang WS, Metcalf CA, Sundaramoorthi R, Wang Y, Zou D, Thomas RM, Zhu X, Cai L, Wen D, Liu S, Romero J, Qi J, Chen I, Banda G, Lentini SP, Das S, Xu Q, Keats J, Wang F, Wardwell S, Ning Y, Snodgrass JT, Broudy MI, Russian K, Zhou T, Commodore L, Narasimhan NI, Mohemmad QK, Iuliucci J, Rivera VM, Dalgarno DC, Sawyer TK, Clackson T, Shakespeare WC. Huang WS, et al. Among authors: metcalf ca. J Med Chem. 2010 Jun 24;53(12):4701-19. doi: 10.1021/jm100395q. J Med Chem. 2010. PMID: 20513156
AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance.
O'Hare T, Shakespeare WC, Zhu X, Eide CA, Rivera VM, Wang F, Adrian LT, Zhou T, Huang WS, Xu Q, Metcalf CA 3rd, Tyner JW, Loriaux MM, Corbin AS, Wardwell S, Ning Y, Keats JA, Wang Y, Sundaramoorthi R, Thomas M, Zhou D, Snodgrass J, Commodore L, Sawyer TK, Dalgarno DC, Deininger MW, Druker BJ, Clackson T. O'Hare T, et al. Among authors: metcalf ca 3rd. Cancer Cell. 2009 Nov 6;16(5):401-12. doi: 10.1016/j.ccr.2009.09.028. Cancer Cell. 2009. PMID: 19878872 Free PMC article.
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.
Thomas M, Huang WS, Wen D, Zhu X, Wang Y, Metcalf CA, Liu S, Chen I, Romero J, Zou D, Sundaramoorthi R, Li F, Qi J, Cai L, Zhou T, Commodore L, Xu Q, Keats J, Wang F, Wardwell S, Ning Y, Snodgrass JT, Broudy MI, Russian K, Iuliucci J, Rivera VM, Sawyer TK, Dalgarno DC, Clackson T, Shakespeare WC. Thomas M, et al. Among authors: metcalf ca. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3743-8. doi: 10.1016/j.bmcl.2011.04.060. Epub 2011 Apr 22. Bioorg Med Chem Lett. 2011. PMID: 21561767
SAR of carbon-linked, 2-substituted purines: synthesis and characterization of AP23451 as a novel bone-targeted inhibitor of Src tyrosine kinase with in vivo anti-resorptive activity.
Shakespeare WC, Wang Y, Bohacek R, Keenan T, Sundaramoorthi R, Metcalf C 3rd, Dilauro A, Roeloffzen S, Liu S, Saltmarsh J, Paramanathan G, Dalgarno D, Narula S, Pradeepan S, van Schravendijk MR, Keats J, Ram M, Liou S, Adams S, Wardwell S, Bogus J, Iuliucci J, Weigele M, Xing L, Boyce B, Sawyer TK. Shakespeare WC, et al. Chem Biol Drug Des. 2008 Feb;71(2):97-105. doi: 10.1111/j.1747-0285.2007.00615.x. Epub 2008 Jan 3. Chem Biol Drug Des. 2008. PMID: 18179464
SRC homology-2 inhibitors: peptidomimetic and nonpeptide.
Sawyer TK, Bohacek RS, Dalgarno DC, Eyermann CJ, Kawahata N, Metcalf CA 3rd, Shakespeare WC, Sundaramoorthi R, Wang Y, Yang MG. Sawyer TK, et al. Among authors: metcalf ca 3rd. Mini Rev Med Chem. 2002 Oct;2(5):475-88. doi: 10.2174/1389557023405765. Mini Rev Med Chem. 2002. PMID: 12370048 Review.
Novel protein kinase inhibitors: SMART drug design technology.
Sawyer TK, Bohacek RS, Metcalf CA 3rd, Shakespeare WC, Wang Y, Sundaramoorthi R, Keenan T, Narula S, Weigele M, Dalgarno DC. Sawyer TK, et al. Among authors: metcalf ca 3rd. Biotechniques. 2003 Jun;Suppl:2-10, 12-5. Biotechniques. 2003. PMID: 12813899 Review. No abstract available.
Bone-targeted Src kinase inhibitors: novel pyrrolo- and pyrazolopyrimidine analogues.
Sundaramoorthi R, Shakespeare WC, Keenan TP, Metcalf CA 3rd, Wang Y, Mani U, Taylor M, Liu S, Bohacek RS, Narula SS, Dalgarno DC, van Schravandijk MR, Violette SM, Liou S, Adams S, Ram MK, Keats JA, Weigle M, Sawyer TK, Weigele M. Sundaramoorthi R, et al. Among authors: metcalf ca 3rd. Bioorg Med Chem Lett. 2003 Sep 15;13(18):3063-6. doi: 10.1016/s0960-894x(03)00647-4. Bioorg Med Chem Lett. 2003. PMID: 12941334
Bone-targeted 2,6,9-trisubstituted purines: novel inhibitors of Src tyrosine kinase for the treatment of bone diseases.
Wang Y, Metcalf CA 3rd, Shakespeare WC, Sundaramoorthi R, Keenan TP, Bohacek RS, van Schravendijk MR, Violette SM, Narula SS, Dalgarno DC, Haraldson C, Keats J, Liou S, Mani U, Pradeepan S, Ram M, Adams S, Weigele M, Sawyer TK. Wang Y, et al. Among authors: metcalf ca 3rd. Bioorg Med Chem Lett. 2003 Sep 15;13(18):3067-70. doi: 10.1016/s0960-894x(03)00648-6. Bioorg Med Chem Lett. 2003. PMID: 12941335
Bone-targeted pyrido[2,3-d]pyrimidin-7-ones: potent inhibitors of Src tyrosine kinase as novel antiresorptive agents.
Vu CB, Luke GP, Kawahata N, Shakespeare WC, Wang Y, Sundaramoorthi R, Metcalf CA 3rd, Keenan TP, Pradeepan S, Corpuz E, Merry T, Bohacek RS, Dalgarno DC, Narula SS, van Schravendijk MR, Ram MK, Adams S, Liou S, Keats JA, Violette SM, Guan W, Weigele M, Sawyer TK. Vu CB, et al. Among authors: metcalf ca 3rd. Bioorg Med Chem Lett. 2003 Sep 15;13(18):3071-4. doi: 10.1016/s0960-894x(03)00649-8. Bioorg Med Chem Lett. 2003. PMID: 12941336
80 results