Research Topics
| Jayaseharan JohnsamuelSummaryAffiliation: The Ohio State University Country: USA Publications
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Detail Information
Publications
Docking simulation with a purine nucleoside specific homology model of deoxycytidine kinase, a target enzyme for anticancer and antiviral therapyJayaseharan Johnsamuel
Division of Medicinal Chemistry, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA
Bioorg Med Chem 13:4160-7. 2005..While water molecules were essential for docking experiments using dCKc, the absence of water molecules in dCKm did not affect the ability to correctly dock various purine nucleosides...
Synthesis and biological evaluation of neutral and zwitterionic 3-carboranyl thymidine analogues for boron neutron capture therapyYoungjoo Byun
Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, USA
J Med Chem 48:1188-98. 2005..2004, 64, 6280-6286 and 6287-6295). To complete previous structure-activity relationship (SAR) studies, 3-[(closo-o-carboranyl)methyl]thymidine (4) was also synthesized and evaluated...
Boronated thymidine analogues for boron neutron capture therapyB T S Thirumamagal
College of Pharmacy, The Ohio State University, Columbus, Ohio 43120, USA
Nucleosides Nucleotides Nucleic Acids 25:861-6. 2006..The synthesis of these potential boron neutron capture therapy (BNCT) agents and their preliminary biological evaluation is described...
Hydrophilically enhanced 3-carboranyl thymidine analogues (3CTAs) for boron neutron capture therapy (BNCT) of cancerSureshbabu Narayanasamy
College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA
Bioorg Med Chem 14:6886-99. 2006..Therefore, it may have the potential to replace N5-2OH, the current lead 3CTA, in preclinical studies. An in silico model for the binding of this compound to hTK1 was developed...
3-Carboranyl thymidine analogues (3CTAs) and other boronated nucleosides for boron neutron capture therapyYoungjoo Byun
College of Pharmacy, The Ohio State University, Columbus, OH, USA
Anticancer Agents Med Chem 6:127-44. 2006..This review will analyze design strategies applied for the synthesis of boron-containing nucleosides in general and in particular reference to 3CTAs. Results of biological studies with these molecules will be discussed...
The synthesis and biochemical evaluation of thymidine analogues substituted with nido carborane at the N-3 positionYoungjoo Byun
Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, 422, Parks Hall, 500, West 12th Avenue, The Ohio State University, Columbus, OH 43210, USA
Appl Radiat Isot 61:1125-30. 2004....
Boron-containing nucleosides as potential delivery agents for neutron capture therapy of brain tumorsRolf F Barth
Department of Pathology, The Ohio State University, Columbus, Ohio 43210, USA
Cancer Res 64:6287-95. 2004..Based on these favorable in vitro and in vivo data, neutron capture therapy studies will be initiated using N5-2OH in combination with two non-cell cycle dependent boron delivery agents, boronophenylalanine and sodium borocaptate...
Receptor-targeted liposomal delivery of boron-containing cholesterol mimics for boron neutron capture therapy (BNCT)B T S Thirumamagal
Division of Medicinal Chemistry and Pharmacognosy, The Ohio State University, Columbus, 43210, USA
Bioconjug Chem 17:1141-50. 2006....
Synthesis of ethyleneoxide modified 3-carboranyl thymidine analogues and evaluation of their biochemical, physicochemical, and structural propertiesJayaseharan Johnsamuel
College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA
Bioorg Med Chem 12:4769-81. 2004..In the third group of structural isomers, no significant differences in phosphorylation rates were observed (17-25%). A structure-function hypothesis explaining these results is presented...
Comparative molecular field analysis and comparative molecular similarity indices analysis of human thymidine kinase 1 substratesAchintya K Bandyopadhyaya
Division of Medicinal Chemistry, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA
Bioorg Med Chem 13:1681-9. 2005..Contour maps obtained from CoMFA and CoMSIA models correlated with the experimentally developed SAR...
A convenient method for the computer-aided molecular design of carborane containing compoundsJayaseharan Johnsamuel
College of Pharmacy, The Ohio State University, 500 W 12th Avenue, Columbus, OH 43210, USA
Bioorg Med Chem Lett 13:3213-6. 2003..It is intended as a guide for boron chemists interested in using CAMD of carborane containing agents for medical applications such as BNCT...
Synthesis and biological evaluation of 3'-carboranyl thymidine analoguesJunhua Yan
College of Pharmacy, Ohio State University, Columbus, OH 43210, USA
Bioorg Med Chem Lett 12:2209-12. 2002..Some of the ether-linked 3'-carboranyl thymidine analogues appeared to be slightly unstable under acidic as well as phosphoryl transfer assay conditions and were, if at all, poor substrates for TK1...
Antikinetoplastid antimitotic activity and metabolic stability of dinitroaniline sulfonamides and benzamidesTesmol G George
Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, 43210, USA
Bioorg Med Chem 14:5699-710. 2006....
Evaluation of human thymidine kinase 1 substrates as new candidates for boron neutron capture therapyAshraf S Al-Madhoun
Department of Molecular Biosciences, Division of Veterinary Medical Biochemistry, Swedish University of Agricultural Sciences, Biomedical Center, Uppsala, Sweden
Cancer Res 64:6280-6. 2004..These findings suggest that compound 10 is a promising candidate for selective delivery of boron-10 to malignant cells, and additional in vivo studies are planned to evaluate it for boron neutron capture therapy of brain tumors...
Synthesis of a small library of 3-(carboranylalkyl)thymidines and their biological evaluation as substrates for human thymidine kinases 1 and 2Ashraf S Al-Madhoun
Department of Veterinary Medical Chemistry, Swedish University of Agricultural Sciences, The Biomedical Center, SE-75123 Uppsala, Sweden
J Med Chem 45:4018-28. 2002..Tether lengths of two and five methylene groups in both series gave the highest enzyme activities in the present study. A hypothesis for this result is presented...
