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V. Bavetsias · SciRah

Researcher profile · Semantic Scholar

V. Bavetsias

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V. Bavetsias — researcher profile on SciRah

h-index: 24
Works: 86
Citations: 2,509

Most-cited papers

Aurora Kinase Inhibitors: Current Status and Outlook
V. Bavetsias, S. Linardopoulos
2015Frontiers in Oncology253 citations Open access
Semantic Scholar
Isothiazolones as inhibitors of PCAF and p300 histone acetyltransferase activity
Lindsay Stimson, M. Rowlands, Yvette M Newbatt, N. Smith +10 more
2005Molecular Cancer Therapeutics222 citations Open access
Semantic Scholar
Aurora B overexpression associates with the thyroid carcinoma undifferentiated phenotype and is required for thyroid carcinoma cell proliferation.
Rosanna Sorrentino, S. Libertini, Pierloronzo Pallante, G. Troncone +8 more
2005Journal of Clinical Endocrinology and Metabolism212 citations Open access
Semantic Scholar
Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns
A. Moore, A. Faisal, D. D. de Castro, V. Bavetsias +14 more
2012Leukemia178 citations Open access
Semantic Scholar
Targeting the alpha-folate receptor with cyclopenta[g]quinazoline-based inhibitors of thymidylate synthase.
E. Henderson, V. Bavetsias, D. Theti, Stuart C. Wilson +2 more
2006Bioorganic & Medicinal Chemistry135 citations
Semantic Scholar
BGC 945, a novel tumor-selective thymidylate synthase inhibitor targeted to alpha-folate receptor-overexpressing tumors.
David D Gibbs, D. Theti, N. Wood, M. Green +7 more
2005Cancer Research109 citations Open access
Semantic Scholar
Crystal structure of an Aurora-A mutant that mimics Aurora-B bound to MLN8054: insights into selectivity and drug design.
Charlotte A. Dodson, M. Kosmopoulou, M. Richards, B. Atrash +3 more
2010Biochemical Journal92 citations Open access
Semantic Scholar
The Aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo
A. Faisal, L. Vaughan, V. Bavetsias, Chong-Bo Sun +10 more
2011Molecular Cancer Therapeutics88 citations Open access
Semantic Scholar
8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors
V. Bavetsias, R. Lanigan, G. F. Ruda, B. Atrash +39 more
2016Journal of Medicinal Chemistry87 citations Open access
Semantic Scholar
Design and synthesis of Cyclopenta[g]quinazoline-based antifolates as inhibitors of thymidylate synthase and potential antitumor agents(,).
V. Bavetsias, Jonathan H. Marriott, Camille Melin, R. Kimbell +3 more
2000Journal of Medicinal Chemistry83 citations Open access
Semantic Scholar
Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate.
V. Bavetsias, J. Large, Chong-Bo Sun, N. Bouloc +18 more
2010Journal of Medicinal Chemistry81 citations Open access
Semantic Scholar
Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases.
V. Bavetsias, Chong-Bo Sun, N. Bouloc, J. Reynisson +3 more
2007Bioorganic & Medicinal Chemistry Letters75 citations Open access
Semantic Scholar
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
V. Bavetsias, Simon Crumpler, Chongbo Sun, Sian Avery +17 more
2012Journal of Medicinal Chemistry67 citations Open access
Semantic Scholar
Structure-Based Design of Orally Bioavailable 1H-Pyrrolo[3,2-c]pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1)
S. Naud, I. Westwood, A. Faisal, P. Sheldrake +24 more
2013Journal of Medicinal Chemistry66 citations Open access
Semantic Scholar
Selective delivery of CB300638, a cyclopenta[g]quinazoline-based thymidylate synthase inhibitor into human tumor cell lines overexpressing the alpha-isoform of the folate receptor.
D. Theti, V. Bavetsias, L. Skelton, J. Titley +3 more
2003Cancer Research63 citations
Semantic Scholar
Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity
Florence Chan, Chong-Bo Sun, Meg Perumal, Q. Nguyen +11 more
2007Molecular Cancer Therapeutics61 citations
Semantic Scholar
Synthesis of isothiazol-3-one derivatives as inhibitors of histone acetyltransferases (HATs).
S. Gorsuch, V. Bavetsias, M. Rowlands, G. Aherne +3 more
2009Bioorganic & Medicinal Chemistry56 citations Open access
Semantic Scholar
Aurora Isoform Selectivity: Design and Synthesis of Imidazo [4, 5-b] pyridine Derivatives as Highly
V. Bavetsias, A. Faisal, Simon Crumpler, Nathan Brown +6 more
201347 citations
Semantic Scholar
Assessing histone demethylase inhibitors in cells: lessons learned
S. Hatch, C. Yapp, R. Montenegro, P. Savitsky +23 more
2017Epigenetics & Chromatin42 citations Open access
Semantic Scholar
Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B.
I. Collins, J. Caldwell, T. Fonseca, A. Donald +13 more
2006Bioorganic & Medicinal Chemistry35 citations Open access
Semantic Scholar
TiCl(OiPr)3 and NaBH(OAc)3: an efficient reagent combination for the reductive amination of aldehydes by electron-deficient amines
C. D. Gutierrez, V. Bavetsias, E. Mcdonald
200535 citations
Semantic Scholar
Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells.
N. Bouloc, J. Large, M. Kosmopoulou, Chong-Bo Sun +10 more
2010Bioorganic & Medicinal Chemistry Letters34 citations Open access
Semantic Scholar
Quinazoline Antifolate Thymidylate Synthase Inhibitors: γ-Linked l-d, d-d, and d-l Dipeptide Analogues of 2-Desamino-2-methyl-N10-propargyl-5,8-dideazafolic Acid (ICI 198583)†,‡
V. Bavetsias, A. Jackman, R. Kimbell, W. Gibson +2 more
199626 citations Open access
Semantic Scholar
Quizartinib-resistant FLT3-ITD acute myeloid leukemia cells are sensitive to the FLT3-Aurora kinase inhibitor CCT241736.
A. Moore, A. Faisal, Grace W. Y. Mak, F. Miraki-Moud +14 more
2020Blood Advances24 citations Open access
Semantic Scholar
The design and synthesis of water-soluble analogues of CB30865, a quinazolin-4-one-based antitumor agent.
V. Bavetsias, Lorraine Skelton, F. Yafai, F. Mitchell +3 more
2002Journal of Medicinal Chemistry23 citations Open access
Semantic Scholar
Aurora Isoform Selectivity: Design and Synthesis of Imidazo[4,5-b]pyridine Derivatives as Highly Selective Inhibitors of Aurora-A Kinase in Cells
V. Bavetsias, Amir Faisal, Simon Crumpler, Nathan Brown +16 more
2013Journal of Medicinal Chemistry20 citations Open access
Semantic Scholar
Folate-based inhibitors of thymidylate synthase: synthesis and antitumor activity of gamma-linked sterically hindered dipeptide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583).
V. Bavetsias, Ann L. Jackman, Jonathan H. Marriott, R. Kimbell +3 more
1997Journal of Medicinal Chemistry20 citations Open access
Semantic Scholar
Prodrugs of thymidylate synthase inhibitors: potential for antibody directed enzyme prodrug therapy (ADEPT).
C. Springer, V. Bavetsias, A. Jackman, F. Boyle +3 more
1996Anti-Cancer Drug Design18 citations
Semantic Scholar
Regioselective C2-arylation of imidazo[4,5-b]pyridines.
J. Macdonald, Victoria Oldfield, V. Bavetsias, J. Blagg
2013Organic and biomolecular chemistry17 citations Open access
Semantic Scholar
Microwave-assisted synthesis of 2-aminonicotinic acids by reacting 2-chloronicotinic acid with amines
C. E. Quevedo, V. Bavetsias, E. Mcdonald
200916 citations
Semantic Scholar
CCT245718, a dual FLT3/Aurora A inhibitor overcomes D835Y-mediated resistance to FLT3 inhibitors in acute myeloid leukaemia cells
Muhammad Tariq, Muhammad Furqan, Hira Parveen, Rahim Ullah +5 more
2021British Journal of Cancer15 citations Open access
Semantic Scholar
A Facile Route to Quinazolin-4(3H)-ones Functionalised at the 2-Position
V. Bavetsias
199815 citations
Semantic Scholar
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
Y. Le Bihan, Rachel M. Lanigan, B. Atrash, Mark G. McLaughlin +25 more
2019European journal of medicinal chemistry14 citations Open access
Semantic Scholar
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
V. Bavetsias, Yolanda Pérez-Fuertes, P. McIntyre, B. Atrash +12 more
2015Bioorganic & Medicinal Chemistry Letters14 citations Open access
Semantic Scholar
Synthesis of novel quinazoline-based antifolates with modified glutamate side chains as potential inhibitors of thymidylate synthase and antitumour agents
V. Bavetsias, G. Bisset, R. Kimbell, F. Boyle +1 more
199714 citations
Semantic Scholar
The synthesis and thymidylate synthase inhibitory activity of L-gamma-L-linked dipeptide and L-gamma-amide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583).
G. Bisset, V. Bavetsias, T. J. Thornton, Krzysztof Pawelczak +3 more
1994Journal of Medicinal Chemistry14 citations Open access
Semantic Scholar
Cyclopenta[g]quinazolinone-based inhibitors of thymidylate synthase targeting α-folate receptor overexpressing tumours: synthetic approaches to 4-{N-[(6RS)-2-hydroxymethyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclopenta[g]quinazolin-6-yl]-N-(prop-2-ynyl)amino}benzoic acid
V. Bavetsias, E. Henderson, E. Mcdonald
200711 citations
Semantic Scholar
Nonpolyglutamatable antifolates as inhibitors of thymidylate synthase (TS) and potential antitumour agents.
V. Bavetsias, A. Jackman
1998Current Medicinal Chemistry11 citations
Semantic Scholar
Quinazoline-based thymidylate synthase inhibitors: relationship between structural modifications and polyglutamation.
A. Jackman, R. Kimbell, M. Brown, L. Brunton +5 more
1995Anti-Cancer Drug Design10 citations
Semantic Scholar
Synthesis and profiling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identification of 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition
D. Fearon, I. Westwood, R. van Montfort, R. Bayliss +2 more
2018Bioorganic & Medicinal Chemistry9 citations Open access
Semantic Scholar
ClTi(OiPr)3-promoted reductive amination on the solid phase: combinatorial synthesis of a biaryl-based sulfonamide library.
C. D. Gutierrez, V. Bavetsias, E. Mcdonald
2008Journal of combinatorial chemistry9 citations
Semantic Scholar
Chemoenzymatic preparation of the novel antifolate thymidylate synthase inhibitor N-(4-{N-[(6S)-2-methyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclopenta[g]quinazolin-6-yl]-N-(prop-2-ynyl)amino}benzoyl)-L-glutamic acid and its glutamyl cleavage product
Jonathan H. Marriott, S. Neidle, Z. Matusiak, V. Bavetsias +3 more
19999 citations
Semantic Scholar
2-Pivalamido-3H-pyrimidin-4-one derivatives: convenient pivalamide hydrolysis using Fe(NO3)3 in MeOH
V. Bavetsias, E. Henderson, E. Mcdonald
20048 citations
Semantic Scholar
Cyclopenta[g]quinazoline-based antifolates: the effect of the chirality at the 6-position on the inhibition of thymidylate synthase (TS).
V. Bavetsias, Jonathan H. Marriott, Davinder S. Theti, J. Melin +2 more
2001Bioorganic & Medicinal Chemistry Letters8 citations Open access
Semantic Scholar
Metabolism of the dual FLT-3/Aurora kinase inhibitor CCT241736 in preclinical and human in vitro models: Implication for the choice of toxicology species
F. Wood, S. Shepherd, A. Hayes, Man-Juan Liu +8 more
2019European Journal of Pharmaceutical Sciences7 citations Open access
Semantic Scholar
Pyrido[3,4-d]pyrimidin-4(3H)-one metabolism mediated by aldehyde oxidase is blocked by C2-substitution
A. Hayes, Yi N. Mok, Man-Juan Liu, Ching Thai +8 more
2016Xenobiotica; the fate of foreign compounds in biological systems6 citations Open access
Semantic Scholar
Antifolate chemistry: synthesis of 4-[N-[(6RS)-2-methyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclopenta[g]quinazolin-6-yl]-N-(prop-2-ynyl)amino]benzoic acid via a (propargyl)Co2(CO)6+ complex.
V. Bavetsias, Rainer Clauss, E. Henderson
2003Organic and biomolecular chemistry6 citations
Semantic Scholar
Design and Synthesis of Cyclopenta[g]quinazoline-Based Antifolates as Inhibitors of Thymidylate Synthase and Potential Antitumor Agents.
V. Bavetsias, Jonathan H. Marriott, Camille Melin, R. Kimbell +3 more
20006 citations
Semantic Scholar
Carboxylic acid bioisosteres of γ-linked dipeptide analogues of the folate-based thymidylate synthase (TS) inhibitor, 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583)
V. Bavetsias, A. Jackman, R. Kimbell, F. Boyle +1 more
19965 citations
Semantic Scholar
Convenient Preparation of α-Tert-Butyl N-Blocked Glutamates Through γ-Allyl Ester Protection
V. Bavetsias, G. Bisset, M. Jarman
19954 citations
Semantic Scholar

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