Tagged: natural products
CMD Paper in Bioorganic & Medicinal Chemistry
Congratulations to Han Yueh, Qiwen Gao, and Professors John Porco and Aaron Beeler on their recent paper in Bioorganic & Medicinal Chemistry entitled “A photochemical flow reactor for large scale syntheses of aglain and rocaglate natural product analogues”
Abstract: Herein, we report the development of continuous flow photoreactors for large scale ESIPT-mediated [3 +2]-photocycloaddition of 2-(p-methoxyphenyl)-3-hydroxyflavone and cinnamate-derived dipolarophiles. These reactors can be efficiently numbered up to increase throughput two orders of magnitude greater than the corresponding batch reactions.
CMD Paper in Science Translational Medicine
Congratulations to William Devine, Lauren Brown, and Professor John Porco on their recent paper in Science Translational Medicine entitled “Inhibiting the oncogenic translation program is an effective therapeutic strategy in multiple myeloma.”
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NIH Funds BU-CMD to Develop New Antifungal Compounds
The National Institutes of Health (NIH) has awarded a four-year grant to Center for Molecular Discovery researcher Lauren Brown and collaborators Leah Cowen (University of Toronto) and Luke Whitesell (Whitehead Institute for Biomedical Research at MIT) on "Targeting Hsp90 in crytococcal fungal pathogenesis." The assembled team combines expertise in fungal biology (Cowen), medicinal chemistry (Brown) and pharmacology/experimental therapeutics (Whitesell) with the goal of developing drug-like small-molecule probes for use in studying disease mechanisms of the fungus Cryptococcus.
Invasive Cryptococcus infections pose a grave threat to human health and have enormous economic consequences. Cryptococcal meningitis, the major clinical manifestation of the disease, has a 100% mortatlity rate if left untreated. Even with the best available therapies, mortality rates remain high at 35-40% due to a limited number of drug classes available, and compromised usefulness of these drugs caused by both dose-limiting toxicity and the emergence of high-grade antifungal drug resistance.
In this project, the team will collaborate to develop small molecule chemical compounds to study a critical molecular mechanism that supports both fungal virulence and the onset of drug-resistance. These compounds will also impact clinical care by serving as promising leads for the future development of new, more effective antifungal drugs.
CMD Nature Scientific Reports Paper
Congratulations to Dr. William Devine and Professors Aaron Beeler and John Porco on their paper “Fine-tuning of macrophage activation using synthetic rocaglate derivatives” in Nature Scientific Reports, published April, 2016. This work, on novel activity identified for the rocaglates, was done in collaboration with the Beeler group, the CMD and with our collaborator Igor Kramnik, and coworkers, at the BU NEIDL.
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(CMD Publications #90)
Professor Porco speaks at The 33rd Herbert C. Brown Lectures in Organic Chemistry, Purdue University
Professor Porco spoke at The 33rd Herbert C. Brown Lectures in Organic Chemistry, Purdue University, on April 15, 2016. His talk was entitled “Chemical Synthesis and Biological Studies of the Rocaglates and Derivatives.”
Abstract: The plant genus Aglaia produces a number of secondary metabolites including the cyclopenta[b]benzofuran silvestrol. Cyclopenta[b]benzofuran natural products possess potent anticancer properties due to modulation of the activity of the RNA helicase eukaryotic initiation factor 4A (eIF4A), which is involved in loading ribosomes onto mRNA templates during translation initiation, a step frequently deregulated in cancer. In this presentation, we will describe our efforts to synthesize silvestrol and rocaglate analogues using photocycloaddition of 3-hydroxyflavones with various dipolarophiles, and evaluation of the rocaglates produced as inhibitors of eukaryotic protein translation.
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