Research Topics
| Lloyd KellandSummaryAffiliation: Cranmer Terrace Country: UK Publications
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Detail Information
Publications
Farnesyl transferase inhibitors in the treatment of breast cancerLloyd R Kelland
Department of Bioscience, St Georges Hospital Medical School, Cranmer Terrace, London, SW17 OQS, UK
Expert Opin Investig Drugs 12:413-21. 2003..It is likely that the future clinical direction of FTIs will be as combination therapy, especially with the taxanes, where synergy has been seen in a variety of preclinical studies...
EuroTIDES 2005--Sixth Annual IBC ConferenceLloyd Kelland
Antisoma plc, West Africa House, Hanger Lane, Ealing, London, W5 3QR, UK
IDrugs 9:101-4. 2006
Emerging drugs for ovarian cancerLloyd R Kelland
Antisoma Research Laboratories, St Georges Hospital Medical School, Cranmer Terrace, London, SW17 0QS, UK
Expert Opin Emerg Drugs 10:413-24. 2005..g., 5,6-dimethyl xanthenone 4-acetic acid). At the pre-clinical level, agents being developed to target the phosphatidylinositol 3 kinase/AKT/mTOR pathway, and K-Ras inhibitors, may offer efficacy in the future...
Of mice and men: values and liabilities of the athymic nude mouse model in anticancer drug developmentL R Kelland
Antisoma Research Laboratories, St Georges Hospital Medical School, Cranmer Terrace, London SW17 OQS, UK
Eur J Cancer 40:827-36. 2004..g. inhibitors of the metastatic process and anti-angiogenic strategies as the vasculature is of murine origin)...
Overcoming the immortality of tumour cells by telomere and telomerase based cancer therapeutics--current status and future prospectsLloyd R Kelland
Antisoma Research Laboratories, St Georges Hospital Medical School, Cranmer Terrace, London SW17 OQS, UK
Eur J Cancer 41:971-9. 2005..g., GRN163L) and from the distinct class of those targeting telomeres (e.g., AS1410 based on BRACO19) will enter Phase I clinical trial where clinical benefit from this class of novel drugs will be determined...
Broadening the clinical use of platinum drug-based chemotherapy with new analogues. Satraplatin and picoplatinLloyd Kelland
University College London, Wolfson Institute for Biomedical Research, Cancer Research Technology Development Laboratories, London, UK
Expert Opin Investig Drugs 16:1009-21. 2007..g., the recent approval of the vascular endothelial growth factor monoclonal antibody bevacizumab with carboplatin and paclitaxel in patients with NSCLC)...
The resurgence of platinum-based cancer chemotherapyLloyd Kelland
Cancer Research Technology Development Laboratories, Wolfson Institute for Biomedical Research, University College London, Gower Street, London, WC1E 6BT, UK
Nat Rev Cancer 7:573-84. 2007....
Drug evaluation: ADH-1, an N-cadherin antagonist targeting cancer vascularizationLloyd Kelland
University College London, Cancer Research Technology Development Laboratories, Gower Street, WCV1E 6BT, London, UK
Curr Opin Mol Ther 9:86-91. 2007..By May 2005, ADH-1 was in phase Ib/II clinical trials in Europe and the US, and phase II clinical trials in Canada...
G-quadruplex compounds and cis-platin act synergistically to inhibit cancer cell growth in vitro and in vivoMekala Gunaratnam
CRUK Biomolecular Structure Group, The School of Pharmacy, University of London, 29 39 Brunswick Square, London, WC1N 1AX, UK
Biochem Pharmacol 78:115-22. 2009....
Discovery and development of anticancer aptamersChristopher R Ireson
Antisoma Research Laboratories, London, UK
Mol Cancer Ther 5:2957-62. 2006..In preclinical studies, additional aptamers have been described against several cancer targets, such as tenascin-C, the transcription factor signal transducer and activator of transcription 3, and antiapoptotic and Ku proteins...
SJG-136 (NSC 694501), a novel rationally designed DNA minor groove interstrand cross-linking agent with potent and broad spectrum antitumor activity: part 1: cellular pharmacology, in vitro and initial in vivo antitumor activityJohn A Hartley
Cancer Research UK Drug DNA Interactions Research Group, Department of Oncology, Royal Free and University College Medical School, London, United Kingdom
Cancer Res 64:6693-9. 2004..v. administration. The level of cross-linking persists over a 24-hour period in this tumor in contrast to cross-links produced by conventional cross-linking agents observed over the same time period...
Tumor dose response to the vascular disrupting agent, 5,6-dimethylxanthenone-4-acetic acid, using in vivo magnetic resonance spectroscopyLesley D McPhail
Department of Basic Medical Sciences, St. George's Hospital Medical School and Antisoma Research, Ltd, London, United Kingdom
Clin Cancer Res 11:3705-13. 2005..31)P MRS revealed tumor response to DMXAA at doses below the maximum tolerated dose for mice. Both (31)P and (1)H MRS provide biomarkers of tumor response to DMXAA that could be used in clinical trials...
Evidence for the involvement of p38 MAP kinase in the action of the vascular disrupting agent 5,6-dimethylxanthenone-4-acetic acid (DMXAA)Liangli Zhao
Auckland Cancer Society Research Centre, Faculty of Medical and Health Sciences, University of Auckland, Auckland, New Zealand
Invest New Drugs 25:271-6. 2007..Its action is incompletely understood and we wished to develop an in vitro system to study its effects...
Structure-based design of benzylamino-acridine compounds as G-quadruplex DNA telomere targeting agentsCristina Martins
CRUK Biomolecular Structure Group, The School of Pharmacy, University of London, 29 39 Brunswick Square, London WC1N 1AX, United Kingdom
Bioorg Med Chem Lett 17:2293-8. 2007..Replacement of the previously reported anilino substituents by benzylamino groups results in enhanced quadruplex interaction, and for one compound, superior telomerase inhibitory activity...
Acquired cellular resistance to flavopiridol in a human colon carcinoma cell line involves up-regulation of the telomerase catalytic subunit and telomere elongation. Sensitivity of resistant cells to combination treatment with a telomerase inhibitorChristopher M Incles
The School of Pharmacy, 29 39 Brunswick Square, London WC1N 1AX, UK
Mol Pharmacol 64:1101-8. 2003....
Overexpression of BclXL in a human ovarian carcinoma cell line: paradoxic effects on chemosensitivity in vitro versus in vivoPaul M Rogers
CRC Centre for Cancer Therapeutics, The Institute of Cancer Research, Sutton, Surrey, United Kingdom
Int J Cancer 97:858-63. 2002..Such effects may be missed in vitro when using short-term growth inhibition or clonogenic assays...
A G-quadruplex-interactive potent small-molecule inhibitor of telomerase exhibiting in vitro and in vivo antitumor activitySharon M Gowan
Cancer Research Campaign (CRC) Center for Cancer Therapeutics, Institute of Cancer Research, Surrey, United Kingdom
Mol Pharmacol 61:1154-62. 2002....
Synthesis and biological evaluation of an N10-Psec substituted pyrrolo[2,1-c][1,4]benzodiazepine prodrugJane M Berry
CRUK Gene Targeted Drug Design Research Group, Cancer Research Laboratories, School of Pharmaceutical Sciences, University of Nottingham, University Park, NG7 2RD, Nottingham, UK
Bioorg Med Chem Lett 12:1413-6. 2002..This prototype could lead to a new generation of clinically useful N10-protected PBD prodrugs...
Establishment and characterization of acquired resistance to the farnesyl protein transferase inhibitor R115777 in a human colon cancer cell lineVictoria Smith
CRC Centre for Cancer Therapeutics, The Institute of Cancer Research, Sutton SM2 5NG, UK
Clin Cancer Res 8:2002-9. 2002..The results suggest that the development of clinical resistance may occur with farnesyl protein transferase inhibitors...
Rat tumor response to the vascular-disrupting agent 5,6-dimethylxanthenone-4-acetic acid as measured by dynamic contrast-enhanced magnetic resonance imaging, plasma 5-hydroxyindoleacetic acid levels, and tumor necrosisLesley D McPhail
Division of Basic Medical Sciences, St George s, University of London, London, UK
Neoplasia 8:199-206. 2006..The absence of any reduction in K(trans) or IAUGC following treatment with 200 mg/kg, despite a significant increase in 5-HIAA, raises concerns about the utility of established DCE-MRI biomarkers to assess tumor response to DMXAA...
Synthesis and antimelanoma activity of reversed amide analogues of N-acetyl-4-S-cysteaminylphenolKathryn Nicoll
WestCHEM, Department of Chemistry, University of Glasgow, Glasgow G12 8QQ, UK
Oncol Res 16:97-106. 2006..Assays of some of the compounds as substrates for tyrosinase showed that the catechol 18 was the best substrate and that the piperidine derivative 7 was the best substrate of the phenolic compounds synthesized...
Amide-based prodrugs of spermidine-bridged dinuclear platinum. Synthesis, DNA binding, and biological activityAlexander Hegmans
Department of Chemistry, Virginia Commonwealth University, Richmond, VA 23284 2006, USA
J Med Chem 51:2254-60. 2008....
Enhancement of aqueous solubility and stability employing a trans acetate axis in trans planar amine platinum compounds while maintaining the biological profileErin S F Ma
Department of Chemistry, Virginia Commonwealth University, Richmond, Virginia 23284-2006, USA
J Med Chem 48:5651-4. 2005..The new compounds are the first cytotoxic transplatinum compounds containing an N(2)O(2) donor set, similar to carboplatin and oxaliplatin...
Synthesis and antimelanoma activity of sterically congested tertiary amide analogues of N-acetyl-4-S-cysteaminylphenolJillian Ferguson
Department of Chemistry, University of Glasgow, Glasgow G12 8QQ, UK
Oncol Res 15:87-94. 2005..The cyclohexanecarboxamides were better substrates for mushroom tyrosinase (EC 1.14.18.1) than the acetamides...
ErbB2 overexpression in an ovarian cancer cell line confers sensitivity to the HSP90 inhibitor geldanamycinVicki Smith
CRC Center for Cancer Therapeutics, The Institute of Cancer Research, Sutton, UK
Anticancer Res 22:1993-9. 2002..These data suggest that erbB2 status in ovarian cancr may contribute to chemosensitivity, in some cases leading to increased sensitivity (as with geldanamycin) but in other cases leading to resistance (as with cisplatin)...
Chemical synthesis and cytotoxicity of dihydroxylated cyclopentenone analogues of neocarzinostatin chromophoreMichael D Urbaniak
Center for Biomolecular Design and Drug Development, School of Chemistry, University of Sussex, Falmer, Brighton, BN1 9QJ, UK
Bioorg Med Chem Lett 13:2025-7. 2003..Those compounds containing a cyclopentenone moiety were active, with the carbonyl group being essential for biological activity...
Synthesis and antimelanoma activity of tertiary amide analogues of N-acetyl-4-S-cysteaminylphenolVikki C Pearson
Department of Chemistry, University of Glasgow, Glasgow G12 8QQ, UK
Oncol Res 13:503-12. 2003..The moderate activity of 13-16 against SK-Mel-24 (non-tyrosinase containing) and an ovarian cell line suggests that interference with the melanin pathway may not be the only mode of action of these new compounds...
Trisubstituted acridine derivatives as potent and selective telomerase inhibitorsR John Harrison
Cancer Research UK Biomolecular Structure Group, The School of Pharmacy, University of London, 29-39 Brunswick Square, London, WC1N 1AX, U.K
J Med Chem 46:4463-76. 2003..These data support a model for the action of these compounds that involves the stabilization of intermediate quadruplex structures that inhibit the elongation of telomeric DNA by telomerase in tumor cells...
Bioreductive prodrugs for cancer therapyBeatrice Seddon
Cancer Research UK Centre for Cancer Therapeutics, Institute of Cancer Research, Sutton, Surrey, UK
Methods Mol Med 90:515-42. 2004
Synthesis and biological evaluation of novel chloroethylaminoanthraquinones with potent cytotoxic activity against cisplatin-resistant tumor cellsKlaus Pors
Department of Pharmaceutical and Biological Chemistry, School of Pharmacy, 29-39 Brunswick Square, University of London, London WC1N 1AX, UK
J Med Chem 47:1856-9. 2004..All the 1,4-disubstituted chloroethylaminoanthraquinones were potently cytotoxic (nM IC(50)s) against cisplatin-resistant ovarian cancer cell lines...
A G-quadruplex telomere targeting agent produces p16-associated senescence and chromosomal fusions in human prostate cancer cellsChristopher M Incles
Cancer Research UK Biomolecular Structure Group, School of Pharmacy, University of London, 29-39 Brunswick Square, London WC1N 1AX, UK
Mol Cancer Ther 3:1201-6. 2004..We also show that treatment with BRACO-19 causes extensive end-to-end chromosomal fusions, consistent with telomere uncapping...
Evaluation of by disubstituted acridone derivatives as telomerase inhibitors: the importance of G-quadruplex bindingR John Harrison
Cancer Research UK Biomolecular Structure Group, The School of Pharmacy, University of London, 29-39 Brunswick Square, London WC1N 1AX, UK
Bioorg Med Chem Lett 14:5845-9. 2004..It is concluded that telomerase inhibitory activity is a necessary though by itself insufficient property in order for cellular growth arrest to occur at sub-toxic concentrations, and that tight quadruplex binding is also required...
Mechanisms of tumor vascular shutdown induced by 5,6-dimethylxanthenone-4-acetic acid (DMXAA): Increased tumor vascular permeabilityLiangli Zhao
Auckland Cancer Society Research Centre, Faculty of Medical and Health Sciences, University of Auckland, Auckland, New Zealand
Int J Cancer 116:322-6. 2005..DMXAA might be useful clinically to potentiate the vascular permeability of other anticancer modalities such as cytotoxic drugs, antibodies, drug conjugates and gene therapy...
In vitro and in vivo pharmacokinetic-pharmacodynamic relationships for the trisubstituted aminopurine cyclin-dependent kinase inhibitors olomoucine, bohemine and CYC202Florence I Raynaud
Cancer Research UK Centre for Cancer Therapeutics at The Institute of Cancer Research, Haddow Laboratories, Belmont, Sutton, United Kingdom
Clin Cancer Res 11:4875-87. 2005..Such markers may be potentially useful in the clinical development of CYC202 and other cyclin-dependent kinase inhibitors...
Antitumor polycyclic acridines. 8.(1) Synthesis and telomerase-inhibitory activity of methylated pentacyclic acridinium saltsRobert A Heald
Cancer Research Laboratories, School of Pharmaceutical Sciences, University of Nottingham, Nottingham NG7 2RD, UK
J Med Chem 45:590-7. 2002..Compound 12d is soluble in water, stable in the pH range of 5-9, efficiently transported into tumor cells, and is currently the lead structure for further elaboration in this new class of telomerase inhibitor...
