Loma Linda University

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David Weldon, PhD
Assistant Professor, Pharmaceutical and Administrative Sciences
School of Pharmacy
Member, Pharmaceutical Science, SP, Faculty of Graduate Studies
Publications    Scholarly Journals--Published
  • Weldon David J, Saulsbury MD, Goh J, Rowland L, Campbell P, Robinson L, Miller C, Christian J, Amis L, Taylor N, Dill C, Davis W Jr, Evans SL, Brantley E.  One-pot synthesis of cinnamylideneacetophenones and their in vitro cytotoxicity in breast cancer cells.  Bioorg Med Chem Lett. 2014; 24(15), 3381-4.

    ( 8/2014 ) Link...
    A series of cinnamylideneacetophenones were synthesized via a modified Claisen–Schmidt condensation reaction and evaluated for cytotoxicity against breast cancer cells using the Alamar Blue™ assay. Derivatives 17 and 18 bearing a 2-nitro group on the B ring, exhibited sub-micromolar cytotoxicity in MCF-7 cells (IC50 = 71 and 1.9 nM), respectively. Derivative 17 also displayed sub-micromolar (IC50 = 780 nM) cytotoxicity in MDA-MB-468 cells. Additionally, 17 and 18 displayed significantly less cytotoxicity than the chemotherapeutic doxorubicin in non-tumorigenic MCF-10A cells. This study provides evidence supporting the continued development of nitro-substituted cinnamylideneacetophenones as small molecules to treat breast cancer.
  • Weldon David J, Shah F, Chittiboyina AG, Sheri A, Chada RR, Gut J, Rosenthal PJ, Shivakumar D, Sherman W, Desai P, Jung JC, Avery MA.  Synthesis, biological evaluation, hydration site thermodynamics, and chemical reactivity analysis of α-keto substituted peptidomimetics for the inhibition of Plasmodium falciparum. Bioorg Med Chem Lett. 2014; 24(5),1274-9.

    ( 1/2014 ) Link...
    A new series of peptidomimetic pseudo-prolyl-homophenylalanylketones were designed, synthesized and evaluated for inhibition of the Plasmodium falciparum cysteine proteases falcipain-2 (FP-2) and falcipain-3 (FP-3). In addition, the parasite killing activity of these compounds in human blood-cultured P. falciparum was examined. Of twenty-two (22) compounds synthesized, one peptidomimetic comprising a homophenylalanine-based α-hydroxyketone linked Cbz-protected hydroxyproline (39) showed the most potency (IC50 80 nM against FP-2 and 60 nM against FP-3). In silico analysis of these peptidomimetic analogs offered important protein-ligand structural insights including the role, by WaterMap, of water molecules in the active sites of these protease isoforms. The pseudo-dipeptide 39 and related compounds may serve as a promising direction forward in the design of competitive inhibitors of falcipains for the effective treatment of malaria.
  Books and Chapters
  • Medicinal Chemistry for Pharmacy Students - ISBN 9781449626556

    Editors: M. O. Faruk Khan and Ashok Philip

    Chapter X. Diabetes and its Related Therapeutics

    Publication date - Fall 2014

    ( 9/2013 - Present )
  • Medicinal Chemistry for Pharmacy Students - ISBN 9781449626556

    Editors: M. O. Faruk Khan and Ashok Philip

    Chapter X. Diuresis and its Related Therapeutics

    Publication date - Fall 2014

    ( 9/2013 - Present )