Other Anticancer Compounds

Through our own synthesis and screening, and through work with collaborators, we have identified a multitude of other anticancer compounds. These compounds are advancing through mode-of-action studies, and through evaluation of efficacy in animal models of cancer.

LDH-A Inhibition: LDH-A inhibition and other tactics that exploit the Warburg Effect have considerable potential as selective anticancer strategies.

Diagram showing four other anticancer compounds that we have identified.

Related Publications:

  1. Discovery of KRB-456, a KRAS G12D switch-I/II allosteric pocket binder that inhibits the growth of pancreatic cancer patient-derived tumors
    Kazi A, Ranjan A, Kumar MVV, Agianian B, Chavez MG, Vudatha V, Wang, R, Vangipurapu R, Chen L, Kennedy P, Subramanian K, Quirke JCK, Beato F, Underwood P, Fleming JB, Trevino J, Hergenrother PJ, Gavathiotis E, Sebti S
    Cancer Res. Comm. 2023, 3, 2623-2639

    Link to Journal
  1. Target-agnostic P-glycoprotein assessment yields strategies to evade efflux, leading to a BRAF inhibitor with intracranial efficacy
    Kelly, A.M.; Berry, M.R.; Tasker, S.Z.; McKee, S.A.; Fan, T.M.; Hergenrother, P.J.
    J. Am. Chem. Soc. 2022, 144, 12367-12380

    Link to journal
    Article PDF
  1. Novel imidazotetrazine evades known resistance mechanisms and is effective against temozolomide-resistant brain cancer in cell culture
    Svec, R.L; McKee, S.A.; Berry, M.R.; Kelly, A.M.; Fan, T.M.; Hergenrother, P.J.
    ACS Chem. Biol. 2022, 17, 299-313

    Link to journal
    Article PDF
  1. Diverse compounds from pleuromutilin lead to a thioredoxin inhibitor and inducer of ferroptosis
    Llabani, E.; Hicklin, R. W.; Lee, H.-Y.; Motika, S. E.; Crawford, L. A.; Weerapana, E., Hergenrother, P. J.
    Nature Chem. 2019, 11, 521

    Link to journal
    Article PDF
  1. Tunable stability of imidazotetrazines leads to a potent compound for glioblastoma
    Svec, R. L.; Furiassi, L.; Skibinski, C. G.; Fan, T. M.; Riggins, G. J.; Hergenrother, P. J.
    ACS Chem. Biol. 2018, 13, 3206-3216.
    ​
    Link to journal
    Article PDF
  1. A Small Molecule that Induces Intrinsic Pathway Apoptosis with Unparalleled Speed
    Palchaudhuri, R.; Lambrecht, M. J.; Botham, R. C.; Partlow, K. C.; Van Ham, T. J.; Putt, K. S.; Nguyen, L. T.; Kim, S.-H.; Peterson, R. T.; Fan, T. M.; Hergenrother, P. J. 
    Cell Reports 2015, 13, 2027-2036.

    Link to journal
    Article PDF
  1. Total Synthesis, Stereochemical Assignment, and Biological Activity of All Known (–)-Trigonoliimines
    Han, S.; Morrison, K. C.; Hergenrother, P. J.; Movassaghi, M.
    J. Org. Chem. 2014, 79, 473-486.

    Link to journal
    Article PDF
  1. Synthesis and Anticancer Activity of all known (–)-Agelastatin Alkaloids
    Han, S.; Siegel, D. S.; Morrison, K. C.; Hergenrother, P. J.; Movassaghi, M.
    J. Org. Chem. 2013, 78, 11970-11984.

    Link to journal
    Article PDF
  1. Synthesis of (+/-)-Actinophyllic Acid and Analogs: Applications of Cascade Reactions and Diverted Total Synthesis
    Granger, B. A.; Jewett, I, T.; Butler, J. D.; Hua, B.; Knezevic, C. E.; Parkinson, E. I.; Hergenrother, P. J.; Martin, S. F.
    J. Am. Chem. Soc. 2013, 135, 12984-12986.

    Link to journal
    Article PDF
  1. Synthesis and Anticancer Activity of Epipolythiodiketopiperazine Alkaloids
    Boyer, N.; Morrison, K. C.; Kim, J.; Hergenrother, P. J.; Movassaghi, M.
    Chem. Sci. 2013, 4, 1646-1657.

    Link to journal
    Article PDF

    MIT News Highlight
  1. Triphenylmethyl Derivatives Enhances the Anticancer Effect of Immunotoxins
    Risberg, K.; Guldvik, I. J.; Palchaudhuri, R.; Xi, Y.; Ju, J., Fodstad, O.; Hergenrother, P. J.; Andersson, Y. 
    J. Immunother. 2011, 34, 438-447.

    Link to journal
    Article PDF
  1. Cribostatin 6 Induces Death in Cancer Cells Through a Reactive Oxygen Species (ROS)-Mediated Mechanism
    Hoyt, M.T.; Palchaudhuri, R.; Hergenrother, P. J.
    Invest. New Drugs 2011, 29, 562-573.

    Link to journal
    Article PDF

    MDLinx Highlight
  1. A Noncompetitive Small Molecule Inhibitor of Estrogen-regulated Gene Expression and Breast Cancer Cell Growth that Enhances Proteasome-dependent Degradation of Estrogen Receptor α
    Cherian, M. T.; Mao, C.; Aninye, I. O.; Reynolds, P. D.; Schiff, R.; Hergenrother, P. J.; Nordeen, S. K.; Wilson, E. M.; Shapiro, D. J.
    J. Biol. Chem. 2010, 285, 41863-41873.

    Link to journal
    Article PDF
  1. Phenylcinnamides as Novel Antimitotic Agents
    Leslie, B. J.; Holaday, C. R.; Nguyen, T.; Hergenrother, P. J.
    J. Med. Chem. 2010, 53, 3964-3972.

    Link to journal
    Article PDF
  1. N-((1-Benzyl-1H-1,2,3-triazol-4-yl)methyl)arylamide as a New Scaffold that Provides Rapid Access to Antimicrotubule Agents: Synthesis and Evaluation of Antiproliferative Activity Against Select Cancer Cell Lines
    Stefely, J. A.; Palchaudhuri, R.; Miller, P. A.; Peterson, R. J.; Moraski, G. C.; Hergenrother, P. J.; Miller, M. J.
    J. Med. Chem. 2010, 53, 3389-3395.

    Link to journal
    Article PDF
  1. Malaria-Infected Mice Are Cured by a Single Oral Dose of New Dimeric Trioxane Sulfones Having Also Selective and Powerful Anticancer Activity
    Rosenthal, A. S.; Chen, X.; Liu, J.; West, D. C.; Hergenrother, P. J.; Shapiro, T. A; Posner, G. H.
    J. Med. Chem. 2009, 52, 1198-1203.

    Link to journal
    Article PDF
  1. Structure-Activity-Relationship of Triphenylmethylamides, Compounds that Potently Induce Apoptosis in Melanoma Cell Lines
    Palchaudhuri, R.; Hergenrother, P. J.
    Bioorg. Med. Chem. Lett. 2008, 18, 5888-5891.

    Link to journal
    Article PDF
  1. The Complex Role of the Triphenylmethyl Motif in Anti-Cancer Compounds
    Palchaudhuri, R.; Nesterenko, V.; Hergenrother, P. J.
    J. Am. Chem. Soc. 2008, 130, 10274-10274.

    Link to journal
    Article PDF
  1. A Small Molecule, Identified as an Inhibitor of the Binding of Estrogen Receptor a to Estrogen Response Elements Blocks the Estrogen-dependent Growth of Cancer Cells
    Mao, C.; Patterson, N.; Cherian, M.; Aninye, I.; Zhang, C.; Patterson, N.; Cheng, J.; Putt; K. S.; Hergenrother, P. J.; Wilson, E.; Nordeen, S. K.; Shapiro, D. J.
    J. Biol. Chem. 2008, 283, 12819-12830.

    Link to journal
    Article PDF
  1. Chelated Iron Sources are Inhibitors of Psudomonas aeruginosa Biofilms and Distribute Efficiently in an in vitro Model of Drug Delivery to the Human Lung
    Musk, D. J.; Hergenrother, P. J.
    J. Appl. Microbiol. 2008, 105, 380-388.

    Link to journal
    Article PDF
  1. A Novel Synthetic Analogue of a Constituent of Isodon excisus Inhibits Transcription of CYP1A1, -1A2, and -1B1 by Preventing Activation of the Aryl Hydrocarbon Receptor
    Sienkiewicz, P.; Ciolino, H.; Leslie, B. J.; Hergenrother, P. J.; Singletary, K.; Yeh, G. C.
    Carcinogenesis 2007, 28, 1052-1057.

    Link to journal
    Article PDF
  1. The Compound 13-D Selectively Induces Apoptosis in White Blood Cancers Versus Other Cancer Cell Types
    Putt, K. S.; Nesterenko, V.; Dothager, R. S.; Hergenrother, P. J. 
    ChemBioChem 2006, 7, 1916-1922.

    Link to journal
    Article PDF
  1. Obtaining and screening compound collections: A user’s guide and a call to chemists
    Hergenrother, P. J.
    Curr. Opin. Chem. Biol. 2006, 10, 213-218.

    Link to journal
    Article PDF
  1. Synthesis and Identification of Small Molecules that Potently Induce Apoptosis in Melanoma Cell Through G1 Cell Cycle Arrest
    Dothager, R. S.; Putt, K. S.; Allen, B. J.; Leslie, B. J.; Nesterenko, V.; Hergenrother, P. J.
    J. Am. Chem. Soc. 2005, 127, 8686-8696.

    Link to journal
    Article PDF

    Chemical & Engineering News Highlight
  1. Identification from a Combinatorial Library of a Small Molecule that Selectively Induces Apoptosis in Cancer Cells
    Nesterenko, V.; Putt, K. S.; Hergenrother, P. J.
    J. Am. Chem. Soc. 2003, 125, 14672-14673.

    Link to journal
    Article PDF

    Chemical & Engineering News Highlight
Procaspase-3 Activation
PARG Inhibition
Activation by NQO1
ErSO-related Compounds
Chemical Tools