Timothy L. Gialelis

ORCID: 0000-0003-0606-2133
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About
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Research Areas
  • Crystallization and Solubility Studies
  • X-ray Diffraction in Crystallography
  • Click Chemistry and Applications
  • Chemical Synthesis and Analysis
  • Fluorine in Organic Chemistry
  • Advanced biosensing and bioanalysis techniques
  • Monoclonal and Polyclonal Antibodies Research
  • Luminescence and Fluorescent Materials
  • Microbial Natural Products and Biosynthesis
  • Cancer therapeutics and mechanisms
  • Bioactive Compounds and Antitumor Agents
  • Molecular Sensors and Ion Detection

La Trobe University
2020-2024

Abstract Diversity Oriented Clicking (DOC) is a unified click‐approach for the modular synthesis of lead‐like structures through application wide family click transformations. DOC evolved from concept achieving “diversity with ease” , by combining classic C−C π‐bond chemistry recent developments in connective SuFEx‐technologies. We showcase 2‐ S ubstituted‐ A lkynyl‐1‐ ulfonyl F luorides (SASFs) as new class hub concert diverse selection click‐cycloaddition processes. Through selective SASFs...

10.1002/anie.202003219 article EN Angewandte Chemie International Edition 2020-04-17

Abstract SuFEx click chemistry is a powerful method designed for the selective, rapid, and modular synthesis of functional molecules. Classical reactions form stable S−O linkages upon exchange S−F bonds with aryl silyl‐ether substrates, while near‐perfect in their outcome, are sometimes disadvantaged by relatively high catalyst loadings prolonged reaction times. We herein report development accelerated (ASCC), an improved efficient catalytic coupling alkyl alcohols range SuFExable hubs....

10.1002/anie.202112375 article EN Angewandte Chemie International Edition 2021-11-10

The Accelerated SuFEx Click Chemistry (ASCC) protocol, adapted to a 96-well plate format, has been applied the late-stage derivatization of bioactive molecules and array synthesis anticancer agents, showcasing its potential for drug discovery.

10.1039/d3sc05729a article EN cc-by-nc Chemical Science 2024-01-01

Abstract Diversity Oriented Clicking (DOC) is a unified click‐approach for the modular synthesis of lead‐like structures through application wide family click transformations. DOC evolved from concept achieving “diversity with ease” , by combining classic C−C π‐bond chemistry recent developments in connective SuFEx‐technologies. We showcase 2‐ S ubstituted‐ A lkynyl‐1‐ ulfonyl F luorides (SASFs) as new class hub concert diverse selection click‐cycloaddition processes. Through selective SASFs...

10.1002/ange.202003219 article EN Angewandte Chemie 2020-04-17

Exploring organic reactions to construct novel molecules with aggregation-induced emission (AIE) features is an essential branch of AIE research. The fast-paced application materials in various disciplines, including photoelectricity, molecular biology, medicine, and science, has led ever-growing need for new molecules. Unlike the synthesis most "earlier generations" fluorogens (AIEgens) that require tedious harsh reactions, chemists now shift their synthetic focus a selection reliable...

10.1016/j.xcrp.2022.100766 article EN cc-by-nc-nd Cell Reports Physical Science 2022-02-01

Abstract SuFEx click chemistry is a powerful method designed for the selective, rapid, and modular synthesis of functional molecules. Classical reactions form stable S−O linkages upon exchange S−F bonds with aryl silyl‐ether substrates, while near‐perfect in their outcome, are sometimes disadvantaged by relatively high catalyst loadings prolonged reaction times. We herein report development accelerated (ASCC), an improved efficient catalytic coupling alkyl alcohols range SuFExable hubs....

10.1002/ange.202112375 article EN Angewandte Chemie 2021-11-10

We report an improved 4-step semisynthesis of (−)-jerantinine A and (−)-melodinine P from (−)-tabersonine, qualify their potency against TNBC cells confirm they induce oxidative stress. JA also acts as a potent inhibitor nucleotide metabolism.

10.1039/d3md00049d article EN RSC Medicinal Chemistry 2023-01-01

Click chemistry is a method for the rapid synthesis of functional molecules with desirable properties. We report development accelerated SuFEx, powerful click reaction efficient coupling aryl and alkyl alcohols directly SuFExable hubs catalyzed by 2-<i>tert</i>-butyl-1,1,3,3-tetramethylguanidine (BTMG, Barton's base). The new circumvents need to synthesize silyl ether substrates while allowing use sub-stoichiometric catalyst loadings. This made possible through synergistic effect...

10.26434/chemrxiv.13623179 preprint EN cc-by-nc-nd 2021-01-25

Click-Chemie Ein vereinheitlichter Ansatz für die Click-Chemie, genannt diversitätorientiertes Clicking, wird von J. E. Moses et al. im Forschungsartikel auf S. 12560 Synthese diverser Leitstrukturen eingeführt.

10.1002/ange.202083063 article DE Angewandte Chemie 2020-07-13
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