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1

Targeting the α-folate receptor with cyclopenta[g]quinazoline-based inhibitors of thymidylate synthase

Elisa A. Henderson, Vassilios Bavetsias, Davinder S. Theti, Stuart C. Wilson, Rainer Clauss, Ann L. Jackman

Journal:

Bioorganic & Medicinal Chemistry

Year:

2006

Language:

english

File:

PDF, 456 KB

english, 2006

2

ChemInform Abstract: Synthesis of Novel Quinazoline-Based Antifolates with Modified Glutamate Side Chains as Potential Inhibitors of Thymidylate Synthase and Antitumor Agents.

V. BAVETSIAS, G. M. F. BISSET, R. KIMBELL, F. T. BOYLE, A. L. JACKMAN

Journal:

Year:

1998

File:

PDF, 30 KB

1998

3

ChemInform Abstract: Nonpolyglutamatable Antifolates as Inhibitors of Thymidylate Synthase (TS) and Potential Antitumor Agents

V. BAVETSIAS, A. L. JACKMAN

Journal:

Year:

1998

File:

PDF, 25 KB

1998

4

ChemInform Abstract: A Facile Route to Quinazolin-4(3H)-ones Functionalized at the 2-Position.

Journal:

Year:

1999

File:

PDF, 27 KB

1999

5

ChemInform Abstract: 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 (Ia) and Its Glutamyl Cleavage Product (Ib).

Jonathan H. Marriott, Stephen Neidle, Zbigniew Matusiak, Vassilios Bavetsias, Ann L. Jackman, Camille Melin, F. Thomas Boyle

Journal:

Year:

1999

File:

PDF, 31 KB

1999

6

ChemInform Abstract: Heterocyclic Templates and Nonpolyglutamatable Inhibitors of Thymidylate Synthase as Potential Antitumor Agents: A Chemical Perspective

Journal:

Year:

2000

File:

PDF, 25 KB

2000

7

ChemInform Abstract: Design and Synthesis of Cyclopenta[g]quinazoline-Based Antifolates as Inhibitors of Thymidylate Synthase and Potential Antitumor Agents.

Vassilios Bavetsias, Jonathan H. Marriott, Camille Melin, Rosemary Kimbell, Zbigniew S. Matusiak, F. Thomas Boyle, Ann L. Jackman

Journal:

Year:

2000

Language:

english

File:

PDF, 29 KB

english, 2000

8

ChemInform Abstract: Synthesis of N-Substituted Derivatives of tert-Butyl 4-Aminobenzoate via a Palladium-Catalyzed Reaction.

V. Bavetsias, E. A. Henderson

Journal:

Year:

2001

File:

PDF, 30 KB

2001

9

2-Pivalamido-3H-pyrimidin-4-one Derivatives: Convenient Pivalamide Hydrolysis Using Fe(NO3)3 in MeOH.

V. Bavetsias, E. A. Henderson, E. McDonald

Journal:

Year:

2004

File:

PDF, 13 KB

2004

10

TiCl(OiPr)3 and NaBH(OAc)3: An Efficient Reagent Combination for the Reductive Amination of Aldehydes by Electron-Deficient Amines.

Corey D. Gutierrez, Vassilios Bavetsias, Edward McDonald

Journal:

Year:

2005

File:

PDF, 18 KB

2005

11

ChemInform Abstract: Microwave-Assisted Synthesis of 2-Aminonicotinic Acids by Reacting 2-Chloronicotinic Acid with Amines.

Camilo E. Quevedo, Vassilios Bavetsias, Edward McDonald

Journal:

Year:

2009

File:

PDF, 22 KB

2009

12

Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B

Ian Collins, John Caldwell, Tatiana Fonseca, Alastair Donald, Vassilios Bavetsias, Lisa-Jane K. Hunter, Michelle D. Garrett, Martin G. Rowlands, G. Wynne Aherne, Thomas G. Davies, Valerio Berdini, Ste

Journal:

Bioorganic & Medicinal Chemistry

Year:

2006

Language:

english

File:

PDF, 570 KB

english, 2006

13

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)

Vassilios Bavetsias, Ann L. Jackman, Rosemary Kimbell, F. Thomas Boyle, Graham M.F. Bisset

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

1996

Language:

english

File:

PDF, 273 KB

english, 1996

14

Synthesis of isothiazol-3-one derivatives as inhibitors of histone acetyltransferases (HATs)

Stephen Gorsuch, Vassilios Bavetsias, Martin G. Rowlands, G. Wynne Aherne, Paul Workman, Michael Jarman, Edward McDonald

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 237 KB

english, 2009

15

Hit generation and exploration: Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases

Vassilios Bavetsias, Chongbo Sun, Nathalie Bouloc, Jóhannes Reynisson, Paul Workman, Spiros Linardopoulos, Edward McDonald

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2007

Language:

english

File:

PDF, 210 KB

english, 2007

16

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

Vassilios Bavetsias, Elisa A. Henderson, Edward McDonald

Journal:

Year:

2007

Language:

english

File:

PDF, 211 KB

english, 2007

17

2-Pivalamido-3H-pyrimidin-4-one derivatives: convenient pivalamide hydrolysis using Fe(NO3)3 in MeOH

V. Bavetsias, E.A. Henderson, E. McDonald

Journal:

Tetrahedron Letters

Year:

2004

Language:

english

File:

PDF, 239 KB

english, 2004

18

TiCl(OiPr)3 and NaBH(OAc)3: an efficient reagent combination for the reductive amination of aldehydes by electron-deficient amines

Corey D. Gutierrez, Vassilios Bavetsias, Edward McDonald

Journal:

Tetrahedron Letters

Year:

2005

Language:

english

File:

PDF, 112 KB

english, 2005

19

Microwave-assisted synthesis of 2-aminonicotinic acids by reacting 2-chloronicotinic acid with amines

Camilo E. Quevedo, Vassilios Bavetsias, Edward McDonald

Journal:

Tetrahedron Letters

Year:

2009

Language:

english

File:

PDF, 744 KB

english, 2009

20

Cyclopenta[g]quinazoline-based antifolates: the effect of the chirality at the 6-position on the inhibition of thymidylate synthase (TS)

V. Bavetsias, J.H. Marriott, D.S. Theti, J.C. Melin, S.C. Wilson, A.L. Jackman

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2001

Language:

english

File:

PDF, 104 KB

english, 2001

21

Synthesis of novel quinazoline-based antifolates with modified glutamate side chains as potential inhibitors of thymidylate synthase and antitumour agents

Vassilios Bavetsias, Graham M.F. Bisset, Rosemary Kimbell, F.Thomas Boyle, Ann L. Jackman

Journal:

Year:

1997

Language:

english

File:

PDF, 822 KB

english, 1997

22

Effect of host lineage on the virulence of Campylobacter jejuni/coli in the chick embryo model

Vicki King, Anita Bavetsia, Nat Bumstead

Journal:

FEMS Microbiology Letters

Year:

1993

Language:

english

File:

PDF, 228 KB

english, 1993

23

Design and Synthesis of Cyclopenta[g]quinazoline-Based Antifolates as Inhibitors of Thymidylate Synthase and Potential Antitumor Agents†,‡

Bavetsias, Vassilios, Marriott, Jonathan H., Melin, Camille, Kimbell, Rosemary, Matusiak, Zbigniew S., Boyle, F. Thomas, Jackman, Ann L.

Journal:

Journal of Medicinal Chemistry

Year:

2000

Language:

english

File:

PDF, 383 KB

english, 2000

24

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, Ray

Journal:

Year:

2012

Language:

english

File:

PDF, 739 KB

english, 2012

25

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

Journal:

Journal of Medicinal Chemistry

Year:

2010

Language:

english

File:

PDF, 2.99 MB

english, 2010

26

The Design and Synthesis of Water-Soluble Analogues of CB30865, a Quinazolin-4-one-Based Antitumor Agent.

V. Bavetsias, L. A. Skelton, F. Yafai, F. Mitchell, S. C. Wilson, B. Allan, A. L. Jackman

Journal:

Year:

2002

File:

PDF, 29 KB

2002

27

ChemInform Abstract: 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. L. JACKMAN, R. KIMBELL, W. GIBSON, F. T. BOYLE, G. M. F. BISSET

Journal:

Year:

1996

Language:

english

File:

PDF, 34 KB

english, 1996

28

The Aurora Kinase Inhibitor CCT137690 Downregulates MYCN and Sensitizes MYCN-Amplified Neuroblastoma In Vivo

Faisal, A., Vaughan, L., Bavetsias, V., Sun, C., Atrash, B., Avery, S., Jamin, Y., Robinson, S. P., Workman, P., Blagg, J.

Journal:

Molecular Cancer Therapeutics

Year:

2011

Language:

english

File:

PDF, 1.00 MB

english, 2011

29

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,

Journal:

Journal of Medicinal Chemistry

Year:

2012

Language:

english

File:

PDF, 2.66 MB

english, 2012

30

Regioselective C2-arylation of imidazo[4,5-b]pyridines

Macdonald, Jonathan, Oldfield, Victoria, Bavetsias, Vassilios, Blagg, Julian

Journal:

Organic & Biomolecular Chemistry

Year:

2013

Language:

english

File:

PDF, 647 KB

english, 2013

31

ClTi(O i Pr) 3 -Promoted Reductive Amination on the Solid Phase: Combinatorial Synthesis of a Biaryl-Based Sulfonamide Library

Gutierrez, Corey D., Bavetsias, Vassilios, McDonald, Edward

Journal:

Journal of Combinatorial Chemistry

Year:

2008

Language:

english

File:

PDF, 333 KB

english, 2008

32

The Design and Synthesis of Water-Soluble Analogues of CB30865, a Quinazolin-4-one-Based Antitumor Agent

Bavetsias, V., Skelton, L. A., Yafai, F., Mitchell, F., Wilson, S. C., Allan, B., Jackman, A. L.

Journal:

Journal of Medicinal Chemistry

Year:

2002

Language:

english

File:

PDF, 170 KB

english, 2002

33

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

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 2.15 MB

english, 2013

34

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,

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 4.51 MB

english, 2013

35

Quinazoline Antifolate Thymidylate Synthase Inhibitors: γ-Linked l - d , d - d , and d - l Dipeptide Analogues of 2-Desamino-2-methyl- N 10 -propargyl-5,8-dideazafolic Acid (ICI 198583) †,‡

Bavetsias, Vassilios, Jackman, Ann L., Kimbell, Rosemary, Gibson, William, Boyle, F. Thomas, Bisset, Graham M. F.

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 572 KB

english, 1996

36

A Facile Route to Quinazolin-4(3 H )-ones Functionalised at the 2-Position

Journal:

Synthetic Communications

Year:

1998

Language:

english

File:

PDF, 471 KB

english, 1998

37

The Synthesis and Thymidylate Synthase Inhibitory Activity of L-.gamma.-L-Linked Dipeptide and L-.gamma.-Amide Analogs of 2-Desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583)

Bisset, Graham M. F., Bavetsias, Vassilios, Thornton, Timothy J., Pawelczak, Krzysztof, Calvert, A. Hilary, Hughes, Leslie R., Jackman, Ann L.

Journal:

Journal of Medicinal Chemistry

Year:

1994

Language:

english

File:

PDF, 1.21 MB

english, 1994

38

Folate-Based Inhibitors of Thymidylate Synthase: Synthesis and Antitumor Activity of γ-Linked Sterically Hindered Dipeptide Analogues of 2-Desamino-2-methyl- N 10 -propargyl-5,8-dideazafolic Acid (ICI 198583) †

Bavetsias, Vassilios, Jackman, Ann L., Marriott, Jonathan H., Kimbell, Rosemary, Gibson, William, Boyle, F. Thomas, Bisset, Graham M. F.

Journal:

Journal of Medicinal Chemistry

Year:

1997

Language:

english

File:

PDF, 807 KB

english, 1997

39

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

Bavetsias, Vassilios, Clauss, Rainer, Henderson, Elisa A.

Journal:

Organic & Biomolecular Chemistry

Year:

2003

Language:

english

File:

PDF, 122 KB

english, 2003

40

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

Marriott, Jonathan H., Neidle, Stephen, Matusiak, Zbigniew, Bavetsias, Vassilios, Jackman, Ann L., Melin, Camille, Boyle, F. Thomas

Journal:

Journal of the Chemical Society Perkin Transactions 1

Year:

1999

Language:

english

File:

PDF, 255 KB

english, 1999

41

Convenient Preparation of α-Tert-Butyl N-Blocked Glutamates Through γ-Allyl Ester Protection

Bavetsias, V., Bisset, G. M. F., Jarman, M.

Journal:

Synthetic Communications

Year:

1995

Language:

english

File:

PDF, 434 KB

english, 1995

42

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

Journal:

Biochemical Journal

Year:

2010

Language:

english

File:

PDF, 1.41 MB

english, 2010

43

Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity

Chan, F., Sun, C., Perumal, M., Nguyen, Q.-D., Bavetsias, V., McDonald, E., Martins, V., Wilsher, N. E., Raynaud, F. I., Valenti, M., Eccles, S., te Poele, R., Workman, P., Aboagye, E. O., Linardopoul

Journal:

Molecular Cancer Therapeutics

Year:

2007

Language:

english

File:

PDF, 522 KB

english, 2007

44

Aurora B Overexpression Associates with the Thyroid Carcinoma Undifferentiated Phenotype and Is Required for Thyroid Carcinoma Cell Proliferation

Sorrentino, Rosanna, Libertini, Silvana, Pallante, Pier Lorenzo, Troncone, Giancarlo, Palombini, Lucio, Bavetsias, Vassilios, Spalletti-Cernia, Daniela, Laccetti, Paolo, Linardopoulos, Spiros, Chieffi

Journal:

Journal of Clinical Endocrinology & Metabolism

Year:

2005

Language:

english

File:

PDF, 483 KB

english, 2005

45

Combinatorial Library of Biaryl-Based Sulfonamides

Gutierrez, C., Bavetsias, V., McDonald, E.

Journal:

Year:

2008

Language:

english

File:

PDF, 76 KB

english, 2008

46

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,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.62 MB

english, 2015

47

8-Substituted Pyrido[3,4- d ]pyrimidin-4(3 H )-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, F

Journal:

Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 2.27 MB

english, 2016

48

Synthesis of N-substituted derivatives of tert-butyl 4-aminobenzoate via a palladium-catalysed reaction

Bavetsias, V., Henderson, E. A.

Journal:

Journal of Chemical Research

Year:

2000

Language:

english

File:

PDF, 34 KB

english, 2000

49

Crystal structure of an Aurora-A mutant that mimics Aurora-B bound to MLN8054: insights into selectivity and drug design

Dodson, C.A., Kosmopoulou, M., Richards, M.W., Atrash, B., Bavetsias, V., Blagg, J., Bayliss, R.

Journal:

Biochemical Journal

Year:

2010

File:

PDF, 22 KB

2010

50

ChemInform Abstract: Regioselective C2-Arylation of Imidazo[4,5-b]pyridines.

Macdonald, Jonathan, Oldfield, Victoria, Bavetsias, Vassilios, Blagg, Julian

Journal:

Year:

2013

File:

PDF, 31 KB

2013