Gustafson Group @ Stony Brook

The S-Atropisomer* had no KIT activity, but displayed intriguing selectivity towards LYN kinase, an emerging target for the treatment of cancer, autoimmune diseases and inflammatory conditions, that currently lacks highly selective inhibitors.

The R-atropisomer* maintained potency against cellular models of GIST (IC50 < 10 nM) while displaying improved target selectivity, including towards key oncogenic c-KIT mutants. *Cahn-Ingold-Prelog priorities cause the analogs to have opposite stereochemical descriptors.*

Another day another preprint on ChemRxiv! “Leveraging Atropisomerism to Obtain a Mutant-Selective c-KIT Inhibitor in Gastrointestinal Stromal Tumors” A story of privileged heterocycles, atropisomerism and kinase selectivity. chemrxiv.org/doi/full/10.26…

This led us to introduce a peri Fluoro group as a H-bonding handle to ‘lock’ that axis into the trans conformation. This seemingly simple modification led to a dramatic increase in HER selectivity, particularly towards HER4, a kinase with emerging implications in ovarian cancer.

The ‘conformational mapping’ of diarylamine crystal structures suggested that the pan-HER kinase inhibitor neratinib adopts two planar conformations around a C–N axes (similar to cis and trans alkenes). HER family kinases generally preferred the ‘trans’ conformation

Excited to share our new ChemRxiv preprint: “Leveraging Conformational Control of Neratinib’s C–N Axes to Enhance HER4 Selectivity in Ovarian Cancer” congrats to the tam @StonyBrookChem and @SDSUChemBiochem Read here: doi.org/10.26434/chemr…

The final version of this manuscript is up at @ACSCatalysis pubs.acs.org/doi/10.1021/ac…

Our department (@StonyBrookChem) is looking for a PRODiG+ fellow – the appointment is two years, followed by conversion to a tenure-track assistant professor at the conclusion of the fellowship. A unique opportunity! apply.interfolio.com/178732

Reposting. One more week until the deadline!

Doctor Gavin Rustin we salute you

Check out our latests work in collaboration with @Taylorlab_Chem ! We evaluated their biomolecular photocaged trifluormethylation reagent on small molecules, finding it effected the rapid trifluoromethylation of diverse aromatics, including several APIs. chemrxiv.org/engage/chemrxi…

The Stony Brook Chemistry Department is searching for a Chemical Biologist at the Associate or Full professor Level. Come join us on Long Island and do some great science! apply.interfolio.com/174211

Professor Jeff Gustafson (Stony Brook University, @GustafsonLab) (gustafsongroup.sdsu.edu/wordpress/) presented the Organic Syntheses Lecture at Notre Dame on September 24th, 2025.

Come join us at @StonyBrookChem! We are looking for an Assoc/Full Prof in Materials or Polymer Chemistry, supported by the SUNY Empire Innovation Program. Deadline Oct 16. Reach out if you have any questions! apply.interfolio.com/173681 #facultychemjobs

Just got back from another excellent Heterocyclic Compounds GRC and am excited to have been elected Vice-Chair. I look forward to putting together an exciting program in 2027! Happy to hear any cool ideas for session topics.

Call for Abstracts: An oral symposium on Synthetically Modified Nucleosides and Nucleic Acids on October 26, 2025 at the @CaliforniaACS Western Regional Meeting in San Jose! Apply, share widely, and DM or email me with questions. wrm2025.org/index.php/prog…

This week marked the Third SBU-BNL Photochemistry Supergroup, with a great poster session and 10 speakers from @StonyBrookChem and MSCE, @BrookhavenLab, @QC_News, @HofstraU, and @AdelphiU! Thanks to @SBUResearch for supporting this event!

here is the correct link: chemrxiv.org/engage/chemrxi…

I am sharing this preprint from my group. Inspired by all the great recent skeletal editing work, we developed an atropisomer selective strategy to take Indoles to quinolines. chemrxiv.org/engage/chemr...

This work was led by Ryan zanolini and Mariam Basilaia. It also involved a fun collaboration with @YuezhiMao that shed light on how stereochemistry was induced (spoiler alert: Dynamic Kinetic Resolution of the indole).