Fadraciclib (CYC065), a novel CDK inhibitor, targets key pro-survival and oncogenic pathways in cancer
Frame, Sheelagh, Saladino, Chiara, MacKay, Craig, Atrash, Butrus, Sheldrake, Peter, McDonald, Edward, Clarke, Paul A, Workman, Paul, Blake, David, Zheleva, Daniella
Published in PloS one (09.07.2020)
Published in PloS one (09.07.2020)
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Structure-Based Design of Orally Bioavailable 1H‑Pyrrolo[3,2‑c]pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1)
Naud, Sébastien, Westwood, Isaac M, Faisal, Amir, Sheldrake, Peter, Bavetsias, Vassilios, Atrash, Butrus, Cheung, Kwai-Ming J, Liu, Manjuan, Hayes, Angela, Schmitt, Jessica, Wood, Amy, Choi, Vanessa, Boxall, Kathy, Mak, Grace, Gurden, Mark, Valenti, Melanie, de Haven Brandon, Alexis, Henley, Alan, Baker, Ross, McAndrew, Craig, Matijssen, Berry, Burke, Rosemary, Hoelder, Swen, Eccles, Suzanne A, Raynaud, Florence I, Linardopoulos, Spiros, van Montfort, Rob L. M, Blagg, Julian
Published in Journal of medicinal chemistry (27.12.2013)
Published in Journal of medicinal chemistry (27.12.2013)
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C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays
Le Bihan, Yann-Vaï, Lanigan, Rachel M., Atrash, Butrus, McLaughlin, Mark G., Velupillai, Srikannathasan, Malcolm, Andrew G., England, Katherine S., Ruda, Gian Filippo, Mok, N. Yi, Tumber, Anthony, Tomlin, Kathy, Saville, Harry, Shehu, Erald, McAndrew, Craig, Carmichael, LeAnne, Bennett, James M., Jeganathan, Fiona, Eve, Paul, Donovan, Adam, Hayes, Angela, Wood, Francesca, Raynaud, Florence I., Fedorov, Oleg, Brennan, Paul E., Burke, Rosemary, van Montfort, Rob L.M., Rossanese, Olivia W., Blagg, Julian, Bavetsias, Vassilios
Published in European journal of medicinal chemistry (01.09.2019)
Published in European journal of medicinal chemistry (01.09.2019)
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Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors
Wilson, Stuart C., Atrash, Butrus, Barlow, Clare, Eccles, Susan, Fischer, Peter M., Hayes, Angela, Kelland, Lloyd, Jackson, Wayne, Jarman, Michael, Mirza, Amin, Moreno, Javier, Nutley, Bernard P., Raynaud, Florence I., Sheldrake, Peter, Walton, Mike, Westwood, Robert, Whittaker, Steven, Workman, Paul, McDonald, Edward
Published in Bioorganic & medicinal chemistry (15.11.2011)
Published in Bioorganic & medicinal chemistry (15.11.2011)
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Journal Article
Assessing histone demethylase inhibitors in cells: lessons learned
Hatch, Stephanie B., Yapp, Clarence, Montenegro, Raquel C., Savitsky, Pavel, Gamble, Vicki, Tumber, Anthony, Ruda, Gian Filippo, Bavetsias, Vassilios, Fedorov, Oleg, Atrash, Butrus, Raynaud, Florence, Lanigan, Rachel, Carmichael, LeAnne, Tomlin, Kathy, Burke, Rosemary, Westaway, Susan M., Brown, Jack A., Prinjha, Rab K., Martinez, Elisabeth D., Oppermann, Udo, Schofield, Christopher J., Bountra, Chas, Kawamura, Akane, Blagg, Julian, Brennan, Paul E., Rossanese, Olivia, Müller, Susanne
Published in Epigenetics & chromatin (01.03.2017)
Published in Epigenetics & chromatin (01.03.2017)
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Fadraciclib
Frame, Sheelagh, Saladino, Chiara, MacKay, Craig, Atrash, Butrus, Sheldrake, Peter, McDonald, Edward, Clarke, Paul A, Workman, Paul, Blake, David, Zheleva, Daniella
Published in PloS one (09.07.2020)
Published in PloS one (09.07.2020)
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Journal Article
8‑Substituted Pyrido[3,4‑d]pyrimidin-4(3H)‑one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors
Bavetsias, Vassilios, Lanigan, Rachel M, Ruda, Gian Filippo, Atrash, Butrus, McLaughlin, Mark G, Tumber, Anthony, Mok, N. Yi, Le Bihan, Yann-Vaï, Dempster, Sally, Boxall, Katherine J, Jeganathan, Fiona, Hatch, Stephanie B, Savitsky, Pavel, Velupillai, Srikannathasan, Krojer, Tobias, England, Katherine S, Sejberg, Jimmy, Thai, Ching, Donovan, Adam, Pal, Akos, Scozzafava, Giuseppe, Bennett, James M, Kawamura, Akane, Johansson, Catrine, Szykowska, Aleksandra, Gileadi, Carina, Burgess-Brown, Nicola A, von Delft, Frank, Oppermann, Udo, Walters, Zoe, Shipley, Janet, Raynaud, Florence I, Westaway, Susan M, Prinjha, Rab K, Fedorov, Oleg, Burke, Rosemary, Schofield, Christopher J, Westwood, Isaac M, Bountra, Chas, Müller, Susanne, van Montfort, Rob L. M, Brennan, Paul E, Blagg, Julian
Published in Journal of medicinal chemistry (25.02.2016)
Published in Journal of medicinal chemistry (25.02.2016)
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Crystal structure of an Aurora-A mutant that mimics Aurora-B bound to MLN8054: insights into selectivity and drug design
Dodson, Charlotte A, Kosmopoulou, Magda, Richards, Mark W, Atrash, Butrus, Bavetsias, Vassilios, Blagg, Julian, Bayliss, Richard
Published in Biochemical journal (01.04.2010)
Published in Biochemical journal (01.04.2010)
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The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo
Faisal, Amir, Vaughan, Lynsey, Bavetsias, Vassilios, Sun, Chongbo, Atrash, Butrus, Avery, Sian, Jamin, Yann, Robinson, Simon P, Workman, Paul, Blagg, Julian, Raynaud, Florence I, Eccles, Suzanne A, Chesler, Louis, Linardopoulos, Spiros
Published in Molecular cancer therapeutics (01.11.2011)
Published in Molecular cancer therapeutics (01.11.2011)
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Aurora Isoform Selectivity: Design and Synthesis of Imidazo[4,5‑b]pyridine Derivatives as Highly Selective Inhibitors of Aurora‑A Kinase in Cells
Bavetsias, Vassilios, Faisal, Amir, Crumpler, Simon, Brown, Nathan, Kosmopoulou, Magda, Joshi, Amar, Atrash, Butrus, Pérez-Fuertes, Yolanda, Schmitt, Jessica A, Boxall, Katherine J, Burke, Rosemary, Sun, Chongbo, Avery, Sian, Bush, Katherine, Henley, Alan, Raynaud, Florence I, Workman, Paul, Bayliss, Richard, Linardopoulos, Spiros, Blagg, Julian
Published in Journal of medicinal chemistry (27.11.2013)
Published in Journal of medicinal chemistry (27.11.2013)
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Journal Article
Structure-Based Design of Orally Bioavailable 1 H -Pyrrolo[3,2- c ]pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1)
Naud, Sébastien, Westwood, Isaac M., Faisal, Amir, Sheldrake, Peter, Bavetsias, Vassilios, Atrash, Butrus, Cheung, Kwai-Ming J., Liu, Manjuan, Hayes, Angela, Schmitt, Jessica, Wood, Amy, Choi, Vanessa, Boxall, Kathy, Mak, Grace, Gurden, Mark, Valenti, Melanie, de Haven Brandon, Alexis, Henley, Alan, Baker, Ross, McAndrew, Craig, Matijssen, Berry, Burke, Rosemary, Hoelder, Swen, Eccles, Suzanne A., Raynaud, Florence I., Linardopoulos, Spiros, van Montfort, Rob L. M., Blagg, Julian
Published in Journal of medicinal chemistry (27.12.2013)
Published in Journal of medicinal chemistry (27.12.2013)
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Metabolism of the dual FLT-3/Aurora kinase inhibitor CCT241736 in preclinical and human in vitro models: Implication for the choice of toxicology species
Wood, Francesca L., Shepherd, Sam, Hayes, Angela, Liu, Manjuan, Grira, Katia, Mok, Yi, Atrash, Butrus, Faisal, Amir, Bavetsias, Vassilios, Linardopoulos, Spiros, Blagg, Julian, Raynaud, Florence I.
Published in European journal of pharmaceutical sciences (01.11.2019)
Published in European journal of pharmaceutical sciences (01.11.2019)
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Journal Article
Optimization of Imidazo[4,5‑b]pyridine-Based Kinase Inhibitors: Identification of a Dual FLT3/Aurora Kinase Inhibitor as an Orally Bioavailable Preclinical Development Candidate for the Treatment of Acute Myeloid Leukemia
Bavetsias, Vassilios, Crumpler, Simon, Sun, Chongbo, Avery, Sian, Atrash, Butrus, Faisal, Amir, Moore, Andrew S, Kosmopoulou, Magda, Brown, Nathan, Sheldrake, Peter W, Bush, Katherine, Henley, Alan, Box, Gary, Valenti, Melanie, de Haven Brandon, Alexis, Raynaud, Florence I, Workman, Paul, Eccles, Suzanne A, Bayliss, Richard, Linardopoulos, Spiros, Blagg, Julian
Published in Journal of medicinal chemistry (25.10.2012)
Published in Journal of medicinal chemistry (25.10.2012)
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Journal Article
Imidazo[4,5-b]pyridine Derivatives As Inhibitors of Aurora Kinases: Lead Optimization Studies toward the Identification of an Orally Bioavailable Preclinical Development Candidates
Bavetsias, Vassilios, Large, Jonathan M., Sun, Chongbo, Bouloc, Nathalie, Kosmopoulou, Magda, Matteucci, Mizio, Wilsher, Nicola E., Martins, Vanessa, Reynisson, Johannes, Atrash, Butrus, Faisal, Amir, Urban, Frederique, Valenti, Melanie, Brandon, Alexis de Haven, Box, Gary, Raynaud, Florence I., Workman, Paul, Eccles, Suzanne A., Bayliss, Richard, Blagg, Julian, Linardopoulos, Spiros, McDonald, Edward
Published in Journal of medicinal chemistry (22.07.2010)
Published in Journal of medicinal chemistry (22.07.2010)
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Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns
Moore, A S, Faisal, A, de Castro, D Gonzalez, Bavetsias, V, Sun, C, Atrash, B, Valenti, M, de Haven Brandon, A, Avery, S, Mair, D, Mirabella, F, Swansbury, J, Pearson, A D J, Workman, P, Blagg, J, Raynaud, F I, Eccles, S A, Linardopoulos, S
Published in Leukemia (01.07.2012)
Published in Leukemia (01.07.2012)
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Journal Article
Imidazo[4,5-b]pyridine Derivatives As Inhibitors of Aurora Kinases: Lead Optimization Studies toward the Identification of an Orally Bioavailable Preclinical Development Candidate
Bavetsias, Vassilios, Large, Jonathan M, Sun, Chongbo, Bouloc, Nathalie, Kosmopoulou, Magda, Matteucci, Mizio, Wilsher, Nicola E, Martins, Vanessa, Reynisson, Jóhannes, Atrash, Butrus, Faisal, Amir, Urban, Frederique, Valenti, Melanie, de Haven Brandon, Alexis, Box, Gary, Raynaud, Florence I, Workman, Paul, Eccles, Suzanne A, Bayliss, Richard, Blagg, Julian, Linardopoulos, Spiros, McDonald, Edward
Published in Journal of medicinal chemistry (22.07.2010)
Published in Journal of medicinal chemistry (22.07.2010)
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Journal Article
7-(Pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine-based derivatives for kinase inhibition: Co-crystallisation studies with Aurora-A reveal distinct differences in the orientation of the pyrazole N1-substituent
Bavetsias, Vassilios, Pérez-Fuertes, Yolanda, McIntyre, Patrick J., Atrash, Butrus, Kosmopoulou, Magda, O’Fee, Lisa, Burke, Rosemary, Sun, Chongbo, Faisal, Amir, Bush, Katherine, Avery, Sian, Henley, Alan, Raynaud, Florence I., Linardopoulos, Spiros, Bayliss, Richard, Blagg, Julian
Published in Bioorganic & medicinal chemistry letters (01.10.2015)
Published in Bioorganic & medicinal chemistry letters (01.10.2015)
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Journal Article
Assessing histone demethylase inhibitors in cells: lessons learned
Hatch, Stephanie B, Yapp, Clarence, Montenegro, Raquel C, Savitsky, Pavel, Gamble, Vicki, Tumber, Anthony, Ruda, Gian Filippo, Bavetsias, Vassilios, Fedorov, Oleg, Atrash, Butrus, Raynaud, Florence, Lanigan, Rachel, Carmichael, LeAnne, Tomlin, Kathy, Burke, Rosemary, Westaway, Susan M, Brown, Jack A, Prinjha, Rab K, Martinez, Elisabeth D, Oppermann, Udo, Schofield, Christopher J, Bountra, Chas, Kawamura, Akane, Blagg, Julian, Brennan, Paul E, Rossanese, Olivia, Müller, Susanne
Published in Epigenetics & chromatin (2017)
Published in Epigenetics & chromatin (2017)
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Pyrido[3,4-d]pyrimidin-4(3H)-one metabolism mediated by aldehyde oxidase is blocked by C2-substitution
Hayes, Angela, Mok, N. Yi, Liu, Manjuan, Thai, Ching, Henley, Alan T., Atrash, Butrus, Lanigan, Rachel M., Sejberg, Jimmy, Le Bihan, Yann-Vaï, Bavetsias, Vassilios, Blagg, Julian, Raynaud, Florence I.
Published in Xenobiotica (02.09.2017)
Published in Xenobiotica (02.09.2017)
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