Sabbir Ahmed

Summary

Affiliation: Kingston University
Country: UK

Publications

  1. ncbi request reprint Novel oxazolidinone based compounds as inhibitors of aromatase and the use of the substrate-heme complex approach in the rationalisation of these compounds
    Sabbir Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston, Surrey, UK
    Biochem Biophys Res Commun 294:380-3. 2002
  2. ncbi request reprint Acid dissociation constant, a potential physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES)
    S Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Kingston upon Thames, Surrey, UK
    Bioorg Med Chem Lett 11:899-902. 2001
  3. ncbi request reprint Determination and use of a transition state for the enzyme estrone sulfatase (ES) from a proposed reaction mechanism
    S Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT1 2EE, UK
    Bioorg Med Chem Lett 11:3001-5. 2001
  4. ncbi request reprint Review of estrone sulfatase and its inhibitors--an important new target against hormone dependent breast cancer
    Sabbir Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey, Surrey, KT1 2EE, UK
    Curr Med Chem 9:263-73. 2002
  5. ncbi request reprint Synthesis and biochemical evaluation of novel and potent inhibitors of the enzyme oestrone sulphatase (ES)
    Sabbir Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT1 2EE, UK
    J Steroid Biochem Mol Biol 80:419-27. 2002
  6. ncbi request reprint Evidence for the mechanism of the irreversible inhibition of oestrone sulphatase (ES) by aminosulphonate based compounds
    Sabbir Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT1 2EE, UK
    J Steroid Biochem Mol Biol 80:429-40. 2002
  7. ncbi request reprint Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES)
    Sabbir Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, KT1 2EE, Surrey, UK
    Bioorg Med Chem Lett 12:1343-6. 2002
  8. ncbi request reprint Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES)
    Sabbir Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT1 2EE, UK
    J Steroid Biochem Mol Biol 82:425-35. 2002
  9. ncbi request reprint The design, synthesis, and biochemical evaluation of derivatives of biphenyl sulfamate-based compounds as novel inhibitors of estrone sulfatase
    Sabbir Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT1 2EE, UK
    Biochem Biophys Res Commun 294:180-3. 2002
  10. ncbi request reprint The use of the novel substrate-heme complex approach in the derivation of a representation of the active site of the enzyme complex 17alpha-hydroxylase and 17,20-lyase
    Sabbir Ahmed
    Department of Pharmacy, School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey, KT1 2EE, UK
    Biochem Biophys Res Commun 316:595-8. 2004

Collaborators

  • Caroline P Owen
  • Abdul Waheed
  • M Patel
  • Chirag K Patel
  • Sachin Dhanani
  • Rupinder K Lota
  • Chirag H Patel
  • Kwabina Aidoo-Gyamfi
  • Imran Shahid
  • Tim Cartledge
  • Kruti Shah
  • Moniola S Olusanjo
  • Karen James
  • Angelique Galisson

Detail Information

Publications39

  1. ncbi request reprint Novel oxazolidinone based compounds as inhibitors of aromatase and the use of the substrate-heme complex approach in the rationalisation of these compounds
    Sabbir Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston, Surrey, UK
    Biochem Biophys Res Commun 294:380-3. 2002
    ..The R-enantiomer based compounds do not protrude in the same area and as such are not thought to undergo any steric hindrance and in comparison to the S-enantiomer, possess greater inhibitory activity...
  2. ncbi request reprint Acid dissociation constant, a potential physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES)
    S Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Kingston upon Thames, Surrey, UK
    Bioorg Med Chem Lett 11:899-902. 2001
    ..We postulate that the stability of the phenoxide ion, as indicated by the acid dissociation constant, is an important factor in the irreversible inhibition of this enzyme...
  3. ncbi request reprint Determination and use of a transition state for the enzyme estrone sulfatase (ES) from a proposed reaction mechanism
    S Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT1 2EE, UK
    Bioorg Med Chem Lett 11:3001-5. 2001
    ..Using the derived structure, we have undertaken the molecular modelling of several steroidal and non-steroidal inhibitors in an attempt to rationalise the inhibitory activity of a number of potent inhibitors...
  4. ncbi request reprint Review of estrone sulfatase and its inhibitors--an important new target against hormone dependent breast cancer
    Sabbir Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey, Surrey, KT1 2EE, UK
    Curr Med Chem 9:263-73. 2002
    ..The review therefore considers the work that has been undertaken to date, as well as possible future development with respect to dual inhibitors of both estrone sulfatase and AR...
  5. ncbi request reprint Synthesis and biochemical evaluation of novel and potent inhibitors of the enzyme oestrone sulphatase (ES)
    Sabbir Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT1 2EE, UK
    J Steroid Biochem Mol Biol 80:419-27. 2002
    ..5 aids the inhibition through the rapid expulsion of the carbon backbone from the active site. We also propose that the same factor is responsible for the hydrolysis of oestrone sulphate reaction, appearing to be an irreversible process...
  6. ncbi request reprint Evidence for the mechanism of the irreversible inhibition of oestrone sulphatase (ES) by aminosulphonate based compounds
    Sabbir Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT1 2EE, UK
    J Steroid Biochem Mol Biol 80:429-40. 2002
    ..Using the results of our SAR study, we postulate the probable mechanism for the irreversible and reversible inhibition of ES, and rationalise the role of the different physicochemical factors in the inhibition of this crucial enzyme...
  7. ncbi request reprint Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES)
    Sabbir Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, KT1 2EE, Surrey, UK
    Bioorg Med Chem Lett 12:1343-6. 2002
    ..Furthermore, the compounds are observed to be irreversible inhibitors...
  8. ncbi request reprint Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES)
    Sabbir Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT1 2EE, UK
    J Steroid Biochem Mol Biol 82:425-35. 2002
    ..Furthermore, the compounds are observed to be irreversible inhibitors...
  9. ncbi request reprint The design, synthesis, and biochemical evaluation of derivatives of biphenyl sulfamate-based compounds as novel inhibitors of estrone sulfatase
    Sabbir Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT1 2EE, UK
    Biochem Biophys Res Commun 294:180-3. 2002
    ....
  10. ncbi request reprint The use of the novel substrate-heme complex approach in the derivation of a representation of the active site of the enzyme complex 17alpha-hydroxylase and 17,20-lyase
    Sabbir Ahmed
    Department of Pharmacy, School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey, KT1 2EE, UK
    Biochem Biophys Res Commun 316:595-8. 2004
    ....
  11. ncbi request reprint The use of the substrate-heme complex approach in the design, synthesis, biochemical evaluation, and rationalization of the inhibitory activity of a range of azole compounds against cholesterol side chain cleavage enzyme
    S Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey, KT1 2EE, United Kingdom
    Biochem Biophys Res Commun 275:75-6. 2000
    ....
  12. ncbi request reprint Structure-activity relationship study of steroidal and nonsteroidal inhibitors of the enzyme estrone sulfatase
    S Ahmed
    School of Applied Chemistry, School of Life Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey, KT1 2EE, United Kingdom
    Biochem Biophys Res Commun 254:811-5. 1999
    ..g., an inhibitor based upon trichloroethanol has been shown to possess 46% inhibition at 0.76mM)...
  13. ncbi request reprint Derivation of a possible transition-state for the reaction catalysed by the enzyme estrone Sulfatase (ES)
    S Ahmed
    School of Applied Chemistry, Kingston University, Kingston upon Thames, Surrey, UK
    Bioorg Med Chem Lett 9:1645-50. 1999
    ..Using the derived structure, we have superimposed several steroidal and non-steroidal inhibitors in an attempt to rationalise the inhibitory activity of a number of potent inhibitors...
  14. ncbi request reprint Design, synthesis, and evaluation of 4-(4'-aminobenzyl)-2-oxazolidinones as novel inhibitors of the cytochrome P-450 enzyme aromatase
    Sabbir Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT1 2EE, UK
    Bioorg Chem 30:315-31. 2002
    ..The compounds were found, in general, to be more potent than the standard compound, aminoglutethimide (AG), and as such proved to be good lead compounds in the search for more specific AR inhibitors...
  15. ncbi request reprint Synthesis and biochemical evaluation of novel inhibitors of aromatase (AR) using an enhanced representation of the active site of AR derived from the consideration of the reaction mechanism
    S Ahmed
    School of Applied Chemistry, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey, KT1 2EE, United Kingdom
    Biochem Biophys Res Commun 267:356-61. 2000
    ....
  16. ncbi request reprint First report of the investigation into the importance of pK(a) in the inhibition of estrone sulfatase by sulfamate containing compounds
    S Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Kingston upon Thames, Surrey, United Kingdom
    Biochem Biophys Res Commun 272:583-5. 2000
    ..The results of the study suggest that there is a strong correlation between the inhibitory activity and the stability of the resulting O(-) anion (i.e., the pK(a) of the starting phenol)...
  17. ncbi request reprint The use of the novel substrate-heme complex approach in the derivation of a representation of the active site of the enzyme cholesterol side chain cleavage
    S Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Surrey, Kingston upon Thames, KT1 2EE, United Kingdom
    Biochem Biophys Res Commun 274:821-4. 2000
    ..Using the derived model, we have rationalised the inhibitory activity of a number of compounds including aminoglutethimide and pyridoglutethimide and the enantiomers of ketoconazole...
  18. doi request reprint Synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a range of 4-hydroxyphenyl ketones as potent and specific inhibitors of the type 3 of 17beta-hydroxysteroid dehydrogenase (17beta-HSD3)
    Rupinder K Lota
    Department of Pharmacy, School of Pharmacy and Chemistry, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey, KT1 2EE, United Kingdom
    J Steroid Biochem Mol Biol 111:128-37. 2008
    ..We have therefore provided good lead compounds in the design and synthesis of novel non-steroidal inhibitors of 17beta-HSD3...
  19. doi request reprint Synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a range of phenyl alkyl imidazole-based compounds as potent inhibitors of the enzyme complex 17alpha-hydroxylase/17,20-lyase (P450(17alpha))
    Caroline P Owen
    Department of Pharmacy, School of Pharmacy and Chemistry, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT1 2EE, UK
    J Steroid Biochem Mol Biol 111:117-27. 2008
    ..We therefore concluded that the azole-based compounds synthesised within the current study are not suitable for further consideration as potential drug candidates due to their lack of specificity...
  20. ncbi request reprint Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid
    Chirag K Patel
    Department of Pharmacy, School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT1 2EE, UK
    Bioorg Med Chem Lett 14:605-9. 2004
    ..The results of the study show that the synthesised compounds possess potent inhibitory activity, indeed the cyclooctyl derivative was found to be more potent than 667-COUMATE, which is currently undergoing clinical trials...
  21. ncbi request reprint The derivation of a potential transition state for the reduction reaction catalysed by 17beta-hydroxysteroid dehydrogenase--an approximate representation of its active site for use in drug design and discovery
    Caroline P Owen
    Department of Pharmacy, School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT1 2EE, UK
    Biochem Biophys Res Commun 318:131-4. 2004
    ..The model is therefore a good start point for the development of novel inhibitors of 17beta-HSD and is a rapid technique for drug design and development...
  22. ncbi request reprint The design, synthesis, and in vitro biochemical evaluation of a series of esters of 4-[(aminosulfonyl)oxy]benzoate as novel and highly potent inhibitors of estrone sulfatase
    Chirag K Patel
    Department of Pharmacy, School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT1 2EE, UK
    Biochem Biophys Res Commun 307:778-81. 2003
    ....
  23. ncbi request reprint A novel steroidal saponin glycoside from Fagonia indica induces cell-selective apoptosis or necrosis in cancer cells
    Abdul Waheed
    School of Pharmacy and Chemistry, Kingston University London, Kingston upon Thames, United Kingdom
    Eur J Pharm Sci 47:464-73. 2012
    ..We conclude that the steroidal saponin glycoside isolated from F. indica is able to induce apoptosis or necrosis in cancer cells depending on the cell type...
  24. doi request reprint Synthesis, biochemical evaluation of a range of potent 4-substituted phenyl alkyl imidazole-based inhibitors of the enzyme complex 17alpha-Hydroxylase/17,20-Lyase (P45017alpha)
    Imran Shahid
    Department of Pharmacy, School of Pharmacy and Chemistry, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT1 2EE, UK
    J Steroid Biochem Mol Biol 110:18-29. 2008
    ....
  25. ncbi request reprint Synthesis and biochemical evaluation of some novel benzoic acid based esters as potential inhibitors of oestrone sulphatase
    Caroline Owen
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT1 2EE, UK
    J Pharm Pharmacol 55:85-93. 2003
    ....
  26. ncbi request reprint Structure-activity relationship determination within a group of substituted phenyl sulfamate based compounds against the enzyme oestrone sulfatase
    Chirag K Patel
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey, KT1 2EE, UK
    J Pharm Pharmacol 55:211-8. 2003
    ....
  27. ncbi request reprint Synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a range of 4-substituted phenyl alkyl imidazole-based inhibitors of the enzyme complex 17alpha-hydroxylase/17,20-lyase (P450(17alpha))
    Chirag H Patel
    Department of Pharmacy, School of Pharmacy and Chemistry, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey, KT1 2EE, UK
    Bioorg Med Chem Lett 16:4752-6. 2006
    ..Modelling of these compounds suggests that the length of the alkyl chain enhances the interaction between the inhibitor and the area of the active site corresponding to the C3 area of the steroid backbone, thereby increasing potency...
  28. ncbi request reprint Inhibition of estrone sulfatase (ES) by derivatives of 4-[(aminosulfonyl)oxy] benzoic acid
    Sabbir Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Kingston upon Thames, Surrey, UK
    Bioorg Med Chem Lett 12:2391-4. 2002
    ..Furthermore, the data suggest a strong correlation between logP and IC(50) and therefore adds further support to our previous report where we suggested a link between inhibitory activity and hydrophobicity...
  29. ncbi request reprint The mechanism of the irreversible inhibition of estrone sulfatase (ES) through the consideration of a range of methane- and amino-sulfonate-based compounds
    Sabbir Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Surrey, KT1 2EE, Kingston upon Thames, UK
    Bioorg Med Chem Lett 12:1279-82. 2002
    ....
  30. ncbi request reprint Estrone sulfatase and its inhibitors
    Kwabina Aidoo-Gyamfi
    Department of Pharmacy, School of Pharmacy and Chemistry, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT12EE, UK
    Anticancer Agents Med Chem 9:599-612. 2009
    ..The review therefore summarises the work that has been undertaken todate...
  31. ncbi request reprint Synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a series of 4-hydroxyphenyl ketones as potential inhibitors of 17beta-hydroxysteroid dehydrogenase type 3 (17beta-HSD3)
    Rupinder K Lota
    Department of Pharmacy, School of Pharmacy and Chemistry, Kingston University, Kingston upon Thames, Surrey, UK
    Bioorg Med Chem Lett 16:4519-22. 2006
    ..86 +/- 0.03 microM). We have therefore provided good lead compounds in the synthesis of novel non-steroidal inhibitors of 17beta-HSD3...
  32. ncbi request reprint Synthesis and biochemical evaluation of a range of potent benzyl imidazole-based compounds as potential inhibitors of the enzyme complex 17alpha-hydroxylase/17,20-lyase (P450(17alpha))
    Caroline P Owen
    Department of Pharmacy, School of Pharmacy and Chemistry, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT1 2EE, UK
    Bioorg Med Chem Lett 16:4011-5. 2006
    ..66+/-0.15 microM against lyase). Furthermore, the compounds tested are less potent towards the 17alpha-OHase component, a desirable property in the development of novel inhibitors of P450(17alpha)...
  33. ncbi request reprint A novel molecular modelling study of inhibitors of the 17alpha-hydroxylase component of the enzyme system 17alpha-hydroxylase/17,20-lyase (P-450(17alpha))
    S Ahmed
    School of Applied Chemistry, Kingston University, Kingston upon Thames, UK
    Bioorg Med Chem 7:1487-96. 1999
    ..Overall, the study suggests that the novel substrate-heme complex approach has provided a good approximation of the 17alpha-OHase active site and has proved to be a useful tool in drug design and discovery...
  34. ncbi request reprint Novel inhibitors of the enzyme estrone sulfatase (ES)
    S Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Kingston upon Thames, Surrey, UK
    Bioorg Med Chem Lett 11:841-4. 2001
    ..The results of the study show that these compounds are potent inhibitors, possessing greater inhibitory activity than COUMATE, but weaker activity than EMATE. Furthermore, the compounds are observed to be irreversible inhibitors...
  35. ncbi request reprint Mechanism based representation of the active site of 5 alpha-reductase (5AR)
    S Ahmed
    School of Applied Chemistry, Kingston University, Kingston upon Thames, Surrey, UK
    Bioorg Med Chem Lett 8:2615-70. 1998
    ....
  36. ncbi request reprint Mechanism of 17 alpha-hydroxylase/17,20-lyase--an initial geometric perspective for the lyase of the C(17)-C(20) bond of C21 steroids
    S Ahmed
    School of Applied Chemistry, Kingston University, Kingston upon Thames, Surrey, UK
    Bioorg Med Chem Lett 8:1023-8. 1998
    ....
  37. ncbi request reprint Hydrophobicity, a physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES)
    S Ahmed
    School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, KT1 2EE, Surrey, UK
    Bioorg Med Chem Lett 11:2525-8. 2001
    ..Analysis of the SAR data shows a strong correlation between IC(50) and logP but also supports our previous study, which suggests a very strong relationship between pK(a) and IC(50)...
  38. ncbi request reprint Structure activity relationship study of known inhibitors of the enzyme 5 alpha-reductase (5AR)
    S Ahmed
    School of Applied Chemistry, Kingston University, Surrey
    Bioorg Med Chem Lett 8:409-14. 1998
    ....
  39. doi request reprint Novel acylated steroidal glycosides from Caralluma tuberculata induce caspase-dependent apoptosis in cancer cells
    Abdul Waheed
    School of Pharmacy and Chemistry, Kingston University, Penryhn Road, Kingston upon Thames, Surrey KT1 2EE, London, United Kingdom
    J Ethnopharmacol 137:1189-96. 2011
    ..The aim of the study was to isolate, using an activity-guided fractionation approach, novel pregnane glycosides for testing on breast cancer and other tumour lines...