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  • Biomimetic synthesis of meroterpenoids by dearomatization-driven polycyclization 

    Powers, Zachary; Scharf, Adam; Cheng, Andrea; Yang, Feng; Himmelbauer, Martin; Mitsuhashi, Takaaki; Barra, Lena; Taniguchi, Yoshimasa; Kikuchi, Takashi; Fujita, Makoto; Abe, Ikuro; Porco, John A. (2019-11-04)
    A biomimetic route to farnesyl pyrophosphate and dimethyl orsellinic acid (DMOA)-derived meroterpenoid scaffolds has yet to be reported despite great interest from the chemistry and biomedical research communities. A concise ...
  • Amidino-rocaglates: a potent class of eIF4A inhibitors 

    Chu, Jennifer; Zhang, Wenhan; Cencic, Regina; Devine, William G.; Beglov, Dmitri; Henkel, Thomas; Brown, Lauren E.; Vajda, Sandor; Porco, John A.; Pelletier, Jerry (2019-11-21)
    Rocaglates share a common cyclopenta[b]benzofuran core that inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase, eIF4A. Working as interfacial inhibitors, rocaglates stabilize the ...
  • Gold(I)-mediated cycloisomerization/cycloaddition enables bioinspired syntheses of neonectrolides B-E and analogues 

    Purgett, Thomas J.; Dyer, Matthew W.; Bickel, Bryce; McNeely, James; Porco, John A. (2019-09-25)
    Development of a synthetic route to the oxaphenalenone (OP) natural products neonectrolides B-E is described. The synthesis relies on gold-catalyzed 6-endo-dig hydroarylation of an unusual enynol substrate as well as a ...
  • Exploiting the potential of meroterpenoid cyclases to expand the chemical space of fungal meroterpenoids 

    Abe, Ikuro; Mitsuhashi, Takaaki; Barra, Lena; Powers, Zachary; Kojasoy, Volga; Cheng, Andrea; Yang, Feng; Taniguchi, Yoshimasa; Kikuchi, Takashi; Fujita, Makoto; Tantillo, Dean J.; Porco, John A. (2020-09-15)
    Fungal meroterpenoids are a diverse group of hybrid natural products with impressive structural complexity and high potential as drug candidates. In this work, we evaluate the promiscuity of the early structure ...
  • Acylphloroglucinols with acetylcholinesterase inhibitory effects from the fruits of Eucalyptus robusta 

    Liu, Hui; He, Xiao-Zhi; Feng, Mi-Yan; Yuan-Zeng; Rauwolf, Tyler J.; Shao, Li-Dong; Ni, Wei; Yan, Hui; Porco, John A.; Hao, Xiao-Jiang; Qin, Xu-Jie; Liu, Hai-Yang (2020-10)
    Eleven new acylphloroglucinols, including six new formylated phloroglucinol-monoterpene meroterpenoids, eucalyprobusals A-F (1-6), one monomeric acylphloroglucinol, eucalyprobusone B (7), and four dimeric acylphloroglucinols, ...
  • Intercepted retro-Nazarov reaction: syntheses of amidino-rocaglate derivatives and their biological evaluation as eIF4A inhibitors 

    Zhang, Wenhan; Chu, Jennifer; Cyr, Andrew M.; Yueh, Han; Brown, Lauren E.; Wang, Tony T.; Pelletier, Jerry; Porco, John A. (2019-08-14)
    Rocaglates are a family of natural products isolated from the genus Aglaia which possess a highly substituted cyclopenta[b]benzofuran skeleton and inhibit cap-dependent protein synthesis. Rocaglates are attractive compounds ...
  • Tracing MYC expression for small molecule discovery 

    Steinberger, Jutta; Robert, Francis; Hallé, Maxime; Williams, David E.; Cencic, Regina; Sawhney, Neha; Pelletier, Dylan; Williams, Philip; Igarashi, Yasuhiro; Porco Jr., John A.; Rodriguez, Abimael D.; Kopp, Brigitte; Bachmann, Brian; Andersen, Raymond J.; Pelletier, Jerry (Cell Press, 2019-05-16)
    Our inability to effectively "drug" targets such as MYC for therapeutic purposes requires the development of new approaches. We report on the implementation of a phenotype-based assay for monitoring MYC expression in ...
  • Regiodivergent photocyclization of dearomatized acylphloroglucinols: asymmetric syntheses of (—)-nemorosone and (—)-6-epi-garcimultiflorone A 

    Wen, Saishuai; Boyce, Jonathan H.; Kandappa, Sunil K.; Sivaguru, Jayaraman; Porco, Jr., John A. (ACS Publications, 2019-07-17)
    Regiodivergent photocyclization of dearomatized acylphloroglucinol substrates has been developed to produce type A polycyclic polyprenylated acylphloroglucinol (PPAP) derivatives using an excited-state intramolecular proton ...
  • Translation inhibition by rocaglates activates a species-specific cell death program in the emerging fungal pathogen Candida auris 

    Iyer, Kali R.; Whitesell, Luke; Porco, Jr., John A.; Henkel, Thomas; Brown, Lauren E.; Robbins, Nicole; Cowen, Leah E. (American Society for Microbiology, 2020-03-10)
    Fungal infections are a major contributor to infectious disease-related deaths worldwide. Recently, global emergence of the fungal pathogen Candida auris has caused considerable concern because most C. auris isolates are ...
  • Rocaglates induce gain-of-function alterations to eIF4A and eIF4F 

    Chu, Jennifer; Zhang, Wenhan; Cencic, Regina; O'Connor, Patrick B. F.; Robert, Francis; Devine, William G.; Selznick, Asher; Henkel, Thomas; Merrick, William C.; Brown, Lauren E.; Baranov, Pavel V.; Porco, Jr., John A.; Pelletier, Jerry (Elsevier Inc., 2020-02-25)
    Rocaglates are a diverse family of biologically active molecules that have gained tremendous interest in recent years due to their promising activities in pre-clinical cancer studies. As a result, this family of compounds has ...

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