Recent Research Publications (total of 185):

 

 

    

 

 

 

l      "Design, Synthesis, Protein-Ligand X-ray Structure, and Biological Evaluation of a Series of Novel Macrocyclic Human Immunodeficiency Virus-1 Protease Inhibitors to Combat Drug Resistance" A. K. Ghosh, S. Kulkarni, D. D. Anderson, L. Hong, A. Baldridge, Y.-F. Wang, A. A. Chumanevich, A. Y. Kovalevsky, Y. Tojo, M. Amano, Y. Koh, J. Tang, I. T. Weber and H. Mitsuya.  J. Med. Chem. 2009, ASAP.

 

l      “P-Glycoprotein Mediates Efflux Transport of Darunavir in Human Intestinal Caso-2 and ABCB1 Gene-Transfected Renal LLC-PK1 Cell Lines”  H. Fujimoto, M. Higuchi, H. Watanabe, Y. Koh, A. K. Ghosh, H. Mitsuya, N. Tanoue, A. Hamada and H. Saito. Biol. Pharm. Bull. 2009, 32, 1588-1593.

 

l      "An Asymmetric Total Synthesis of Brevisamide" A. K. Ghosh and J. Li.  Org. Lett. 2009, 11 (18), 4164–4167.

 

l      “Synthesis of Bioactive Natural Products by Asymmetric syn- and anti-Aldol Reactions” A. K. Ghosh and Z. L. Dawson Synthesis, 2009, 2992-3003.

 

l      “Structure-Based Design, Synthesis, and Biological Evaluation of a Series of Novel and Reversible Inhibitors for the Severe Acute Respiratory Syndrome−Coronavirus Papain-Like Protease” A. K. Ghosh, J. Takayama, Y. Aubin, K. Ratia, R. Chaudhuri, Y. Baez, K. Sleeman, M. Coughlin, D. B. Nichols, D. C. Mulhearn, B. S. Prabhakar, S. C. Baker, M. E. Johnson and A. D. Mesecar J. Med. Chem. 2009, 52, 5228-5240.

 

l      "A Symmetry-Based Concise Formal Synthesis of Platencin, a Novel Lead against "Superbugs" " A. K. Ghosh and K. Xi  Angew. Chem. Int. Ed. 2009, 48, 5372-5375.

 

l      "Asymmetric Synthesis of anti-Aldol Segments via a Nonaldol Route: Synthetic Applications to Statines and (-)-Tetrahydrolipstatin" A. K. Ghosh, K. Shurrush, S. Kulkarni J. Org. Chem. 2009, 74, 4508-4518.

 

l      “Design of HIV-1 Protease Inhibitors with Pyrrolidinones and Oxazolidinones as Novel P1’-Ligands to Enhance Backbone-binding interactions with Protease: Synthesis, Biological Evaluation and Protein-ligand X-ray Studies” A. K. Ghosh, S. Leshchenko-Yashchuk,  D. D. Anderson, A. Baldridge, M. Noetzel, H. B. Miller, Y. Tie, Y.-F. Wang, Y. Koh, I. T. Weber, and H. Mitsuya J. Med. Chem. 2009, 52, 3902-3914.

 

l      “A Convergent Synthesis of the Proposed Structure of Antitumor Depsipeptide, Stereocalpin A”" A. K. Ghosh and Chun-Xiao Xu Org. Lett. 2009, 11, 1963-1966.

 

l      “Harnessing Nature’s Insight: Design of Aspartyl Protease Inhibitors from Treatment of Drug-Resistant HIV to Alzheimer’s Disease” A. K. Ghosh J. Med. Chem. 2009, 52(8), 2163-2176.

 

l      "Total Synthesis of (-)-Platensimycin, a Novel Antibacterial Agent” " A. K. Ghosh and Kai Xi, J. Org. Chem. 2009, 74, 1163-1170.

 

l      “Stereoselective synthesis of the C1-C12 segment of iriomoteolide-1a: a very potent macrolide antitumor agent” A. K. Ghosh, Hao Yuan, Tet. Lett., 2009, 50, 1416-1418. 

 

l      “GRL-02031: A Novel Nonpeptide Protease Inhibitor (PI) Containing A Stereochemistry Defined Fused Cyclopentanyltetrahydrofuran (Cp-THF) Potent Against Multi-PI-Resistant HIV-1 In Vitro” Y. Koh, D. Das, S. Leshchenko, H. Nakata, H. Ogata-Aoki, M. Amano, M. Nakayama, A. K. Ghosh, and H. Mitsuya, Antimicrob. Agents Chemother. 2009, 53, 987-996.

 

l      “Design and Synthesis of Stereochemically Defined Novel Spirocyclic P¬2-Ligands for HIV-1 Protease Inhibitors” A. K. Ghosh, B. D. Chapsal, A. Baldridge, K. Ide, Y. Koh, and H. Mitsuya, Org. Lett. 2008, 10, 5135-38.

 

l      “Structural Evidence for Effectiveness of Darunavir and Two Related Antiviral Inhibitors against HIV-2 Protease” A. Y. Kovalevsky, J. M. Louis, A. Aniana, A. K. Ghosh, I. T. Weber J.Mol. Biol. 2008, 384, 178-192.

 

l       “L-Selectride-Mediated Highly Diastereoselective Asymmetric Reductive Aldol Reaction: Access to an Important Subunit for Bioactive Molecules” A. K. Ghosh, J. Kass, D. D. Anderson, X. Xu and C. Marian, Org. Lett. 2008, 10, 4811-14.

 

l      “A noncovalent class of papain-like protease/deubiquitinase inhibitors blocks SARS virus replication” K. Ratia, S. Pegan, J. Takayama, K. Sleeman, M. Coughlin, S. Baliji, R. Chaudhuri, W. Fu, B. S. Prabhakar, M. E. Johnson, S. C. Baker, A. K. Ghosh, and A. D. Mesecar, PNAS, 2008, 105, 16119-16124.

 

l      “Solution Kinetics Measurements Suggest HIV-1 Protease Has Two Binding Sites for Darunavir and Amprenavir” A. Y. Kovalevsky; A. K. Ghosh.; I. T. Weber. J. Med. Chem. 2008, 51, 6599-03.

 

l      “Design, Synthesis and Antiviral Efficacy of a Series of Potent Chloropyridyl Ester-derived SARS-CoV 3CLpro Inhibitors” A. K. Ghosh, G. Gong, V. Grum-Tokars, D. C. Mulhearn, M. Coughlin, B. S. Prabhakar, K. Sleeman, S. C. Baker, M. E. Johnson, and A. D. Mesecar, Bioorg. Med. Chem. Lett. 2008, 18, 5684-5688.

 

l      "Flexible Cyclic Ethers/Polyethers as Novel P2-Ligands for HIV-1 Protease Inhibitors: Design, Synthesis, Biological Evaluation and Protein-ligand X-ray Studies" A. K. Ghosh, S. Gemma, A. Baldridge, Y.-F. Wang, A. Y. Kovalevsky, Y. Koh, I. T. Weber, and H. Mitsuya, J. Med. Chem. 2008, 51, 6021-33.

 

l      "Total Synthesis of Potent Antitumor Agent (-)-Lasonolide A: a Cycloaddition-based Strategy" Arun Ghosh and Gangli Gong, Chem. Asian J. 2008, 3, 1811-1823.

 

l      "Enantioselective Total Synthesis of (+)-Largazole, a Potent Inhibitor of Histone Deacetylase" Arun K. Ghosh, Sarang Kulkarni, Org. Lett. 2008, 10, 3907-09.

 

l      "Effect of Flap Mutations on Structure of HIV-1 Protease and Inhibition by Saquinavir and Darunavir" Fengling Liu, Andrey Y. Kovalevsky, Yunfeng Tie, Arun K. Ghosh, Robert W. Harrison, Irene T. Weber, J. Mol. Biol. 2008, 381, 102-115.   

 

l      “Beta-Secretase as a Therapeutic Target for Alzheimer’s Disease” Arun K. Ghosh, Sandra Gemma, Jordan Tang, Neurotherapeutics, 2008, 5, 399-408.

 

l      “Potent HIV-1 Protease Inhibitors Incorporating meso-Bicyclic Urethanes as P2-ligands: Structure-Based Design, Synthesis, Biological Evaluation and Protein-Ligand X-Ray Studies” Arun K. Ghosh, Sandra Gemma, Jun Takayama, Abigail Baldridge, Sofiya Leshchenko-Yashchuk, Heather B Miller, Yuan-Fang Wang, Andrey Yu. Kovalevsky, Yashiro Koh, Irene T. Weber, and Hiroaki Mitsuya, Org. Biomol. Chem., 2008, 6, 3703-3713.

 

l      "Asymmetric multi-component reactions: convenient access to acyclic stereocenters and functionalized cyclopentenoids" Arun K. Ghosh, Sarang S. Kulkarni, Chun-Xiao Xu, Khriesto Shurrush, Tet. Asy. 2008, 19, 1020-1026.

 

l      “Enantioselective Synthesis of Cyclopentyltetrahydrofuran (Cp-THF), an Important High-Affinity P2-Ligand for HIV-1 Protease Inhibitors” Arun K. Ghosh and Jun Takayama, Tet. Lett. 2008, 49, 3409-3412.  

 

l      “Memapsin 2 (beta-secretase) inhibitors: drug development.” A. K. Ghosh, N. Kumaragurubaran, L. Hong, G. Koelsh, J. Tang.  Curr. Alz. Res.  2008, 5, 121.

 

l      "Design of HIV Protease Inhibitors Targeting Protein Backbone: An Effective Strategy for Combating Drug Resistance" Arun Ghosh, Bruno Chapsal, Irene Weber, Hiroaki Mitsuya, Acc. Chem. Res. 2008, 41, 78-86.

 

l      "Enantioselective total synthesis of Peloruside A, a potent Microtubule Stabilizer" Arun Ghosh, Xiaoming Xu, Jae-Hun Kim, Chun-Xiao Xu, Org. Lett. 2008, 10, 1001.

 

l      "Potent memapsin 2 (beta-secretase) inhibitors: Design, synthesis, protein-ligand X-ray structure, and in vivo evaluation" Arun K. Ghosh, Nagaswamy Kumaragurubaran, Lin Hong, Sarang Kulkarni, Xiaoming Xu, Heather B Miller, Dandepally S Reddy, Vajira Weerasena, Robert Turner, Wanpin Chang, Gerald Koelsch, and Jordan Tang. Bioorg. Med. Chem. Lett. 2008, 18, 1031-1036.

 

 

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