Natural product derived privileged scaffolds in drug discovery

EK Davison, MA Brimble - Current opinion in chemical biology, 2019 - Elsevier
The biological activity and structural diversity of natural products are unsurpassed by any
available synthetic screening libraries. As such, these privileged scaffolds serve as …

Antibody-drug conjugates for targeted cancer therapy: Recent advances in potential payloads

M Xi, J Zhu, F Zhang, H Shen, J Chen, Z Xiao… - European Journal of …, 2024 - Elsevier
Antibody-drug conjugates (ADCs) represent a promising cancer therapy modality which
specifically delivers highly toxic payloads to cancer cells through antigen-specific …

Gold-catalyzed glycosylation in the synthesis of complex carbohydrate-containing natural products

W Li, B Yu - Chemical Society Reviews, 2018 - pubs.rsc.org
The methodological developments in gold (I)-and gold (III)-catalyzed glycosylation reactions
are fully surveyed, which exploit the special alkynophilicity or the Lewis acidity of the gold …

Enantioselective N-Heterocyclic Carbene-Catalyzed Hauser-Kraus Annulations for the Construction of C–N Axially Chiral Phthalimde Derivatives

P Ren, Q Zhao, K Xu, T Zhu - ACS Catalysis, 2024 - ACS Publications
The Hauser-Kraus annulation is one of the most powerful methods to construct polycyclic
hydroquinone from 3-cyano phthalides and Michael acceptors. Although these methods …

Total synthesis in search of potent antibody–drug conjugate payloads. From the fundamentals to the translational

KC Nicolaou, S Rigol - Accounts of Chemical Research, 2018 - ACS Publications
Conspectus The emergence and evolution of antibody–drug conjugates (ADCs) as targeted
cancer therapies in recent years is a living example of the “magic bullet” concept of Paul …

Metabolomics tools assisting classic screening methods in discovering new antibiotics from mangrove actinomycetia in Leizhou Peninsula

QP Lu, YM Huang, SW Liu, G Wu, Q Yang, LF Liu… - Marine drugs, 2021 - mdpi.com
Mangrove actinomycetia are considered one of the promising sources for discovering novel
biologically active compounds. Traditional bioactivity-and/or taxonomy-based methods are …

Streamlined total synthesis of shishijimicin A and its application to the design, synthesis, and biological evaluation of analogues thereof and practical syntheses of …

KC Nicolaou, R Li, Z Lu, EN Pitsinos… - Journal of the …, 2018 - ACS Publications
Shishijimicin A is a scarce marine natural product with highly potent cytotoxicities, making it
a potential payload or a lead compound for designed antibody–drug conjugates. Herein, we …

Advances in the asymmetric total synthesis of natural products using chiral secondary amine catalyzed reactions of α, β-unsaturated aldehydes

Z Wang - Molecules, 2019 - mdpi.com
Chirality is one of the most important attributes for its presence in a vast majority of bioactive
natural products and pharmaceuticals. Asymmetric organocatalysis methods have emerged …

Trioxacarcin A interactions with G-quadruplex DNA reveal its potential new targets as an anticancer agent

S Yin, W Lan, X Hou, Z Liu, H Xue… - Journal of Medicinal …, 2023 - ACS Publications
Trioxacarcin (TXN) A was reported to be an anticancer agent through alkylation of dsDNA. G-
quadruplex DNA (G4-DNA) is frequently formed in the promoter regions of oncogenes and …

Aza-Rubottom oxidation: synthetic access to primary α-aminoketones

Z Zhou, QQ Cheng, L Kürti - Journal of the American Chemical …, 2019 - ACS Publications
An aza analogue of the Rubottom oxidation is reported. This facile transformation takes
place at ambient temperature and directly converts silyl enol ethers to the corresponding …