The main objective of this project is the synthesis of compound libraries based on enantiomerically pure, stereochemically well-defined, novel, versatile, and interesting molecular scaffolds that are derived from or inspired by natural products and privileged structures.
The specific aims of this project are: 1. Prepare a demonstration library based on the eight-membered lactone natural product and powerful antitumor agent octalactin A via ring-closing metathesis (RCM) chemistry and evaluate the analogues for cytotoxic activity against human cancer cell lines. 2. Develop a new class of ionic norbornenyl linkers for combinatorial chemistry. 3. Preparation of trienomycin A analogues by combinatorial methods using both solid- and solution-phase technologies. 4. Utilization of polymer-supported phosphonium salts, olefin cross-metathesis, oligomeric chiral auxiliaries and PEG-supported dioxolanes during the construction of the macrocyclic core of trienomycin A. 5. Development of novel chemistry to prepare unique nitrogen-containing scaffolds. 6. Development of novel traceless linker methodology for solid phase asymmetric synthesis.

National Institute of Health (NIH)
National Institute of General Medical Sciences (NIGMS)
Specialized Center (P50)
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Special Emphasis Panel (ZGM1)
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University of Kansas Lawrence
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Wang, Xuewei; Jolliffe, Aaron; Carr, Benjamin et al. (2018) Nitric oxide-releasing semi-crystalline thermoplastic polymers: preparation, characterization and application to devise anti-inflammatory and bactericidal implants. Biomater Sci 6:3189-3201
Knewtson, Kelsey E; Rane, Digamber; Peterson, Blake R (2018) Targeting Fluorescent Sensors to Endoplasmic Reticulum Membranes Enables Detection of Peroxynitrite During Cellular Phagocytosis. ACS Chem Biol 13:2595-2602
Ramakumar, Kinthada; Maji, Tapan; Partridge, James J et al. (2017) Synthesis of Spirooxindoles via the tert-Amino Effect. Org Lett 19:4014-4017
Faisal, Saqib; Zang, Qin; Maity, Pradip K et al. (2017) Development and Application of a Recyclable High-Load Magnetic Co/C Hybrid ROMP-Derived Benzenesulfonyl Chloride Reagent and Utility of Corresponding Analogues. Org Lett 19:2274-2277
Koen, Yakov M; Liu, Ke; Shinogle, Heather et al. (2016) Comparative Toxicity and Metabolism of N-Acyl Homologues of Acetaminophen and Its Isomer 3'-Hydroxyacetanilide. Chem Res Toxicol 29:1857-1864
Gold, Ben; Smith, Robert; Nguyen, Quyen et al. (2016) Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis. J Med Chem 59:6027-44
Faisal, Saqib; Maity, Pradip K; Zang, Qin et al. (2016) Application of Silica-Supported Alkylating Reagents in a One-Pot, Sequential Protocol to Diverse Benzoxathiazepine 1,1-Dioxides. ACS Comb Sci 18:387-93
Gowthaman, Ragul; Miller, Sven A; Rogers, Steven et al. (2016) DARC: Mapping Surface Topography by Ray-Casting for Effective Virtual Screening at Protein Interaction Sites. J Med Chem 59:4152-70
Faisal, Saqib; Maity, Pradip K; Zang, Qin et al. (2016) Synthesis of High-Load, Hybrid Silica-Immobilized Heterocyclic Benzyl Phosphate (Si-OHBP) and Triazolyl Phosphate (Si-OHTP) Alkylating Reagents. ACS Comb Sci 18:394-8
Loh, Joanna K; Asad, Naeem; Samarakoon, Thiwanka B et al. (2015) Modular, One-Pot, Sequential Aziridine Ring Opening-S(N)Ar Strategy to 7-, 10-, and 11-Membered Benzo-Fused Sultams. J Org Chem 80:9926-41

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