Capturing biological activity in natural product fragments by chemical synthesis

EA Crane, K Gademann - Angewandte Chemie International …, 2016 - Wiley Online Library
Natural products have had an immense influence on science and have directly led to the
introduction of many drugs. Organic chemistry, and its unique ability to tailor natural products …

Synthetic opportunities and challenges for macrocyclic kinase inhibitors

JA Amrhein, S Knapp, T Hanke - Journal of Medicinal Chemistry, 2021 - ACS Publications
Macrocycles are typically cyclic variants of inhibitors derived from uncyclized canonical
molecules or from natural products. For medicinal chemistry, drug-like macrocycles have …

Conformation–activity relationships of polyketide natural products

EM Larsen, MR Wilson, RE Taylor - Natural product reports, 2015 - pubs.rsc.org
Covering: up to the end of 2014 Polyketides represent an important class of secondary
metabolites that interact with biological targets connected to a variety of disease-associated …

Unlocking the drug potential of the bryostatin family: recent advances in product synthesis and biomedical applications

R Wu, H Chen, N Chang, Y Xu, J Jiao… - … –A European Journal, 2020 - Wiley Online Library
Bryostatins are a class of naturally occurring macrocyclic lactones with a unique fast
developing portfolio of clinical applications, including treatment of AIDS, Alzheimer's …

Targeting PKC in microglia to promote remyelination and repair in the CNS

PM Kim, MD Kornberg - Current Opinion in Pharmacology, 2022 - Elsevier
Microglia and CNS-infiltrating macrophages play significant roles in the pathogenesis of
neuroinflammatory and neurodegenerative diseases, such as Alzheimer's disease …

Evaluation of chromane-based bryostatin analogues prepared via hydrogen-mediated C–C bond formation: potency does not confer bryostatin-like biology

JM Ketcham, I Volchkov, TY Chen… - Journal of the …, 2016 - ACS Publications
The synthesis and biological evaluation of chromane-containing bryostatin analogues WN-2–
WN-7 and the previously reported salicylate-based analogue WN-8 are described …

Toward a biorelevant structure of protein kinase C bound modulators: design, synthesis, and evaluation of labeled bryostatin analogues for analysis with rotational …

BA Loy, AB Lesser, D Staveness… - Journal of the …, 2015 - ACS Publications
Protein kinase C (PKC) modulators are currently of great importance in preclinical and
clinical studies directed at cancer, immunotherapy, HIV eradication, and Alzheimer's …

Improved and large-scale synthesis of 10-methyl-aplog-1, a potential lead for an anticancer drug

M Kikumori, RC Yanagita, K Irie - Tetrahedron, 2014 - Elsevier
Methyl-aplog-1 (1), a simplified analog of tumor-promoting aplysiatoxin, is a potential lead
for cancer therapy that exhibits marked and selective growth inhibitory effects against …

Neristatin 1 provides critical insight into bryostatin 1 structure–function relationships

N Kedei, MB Kraft, GE Keck, CL Herald… - Journal of natural …, 2015 - ACS Publications
Bryostatin 1, a complex macrocyclic lactone isolated from Bugula neritina, has been the
subject of multiple clinical trials for cancer. Although it functions as an activator of protein …

Simplified Bryostatin Analogues Protect Cells from Chikungunya Virus-Induced Cell Death

D Staveness, R Abdelnabi, AJ Schrier… - Journal of natural …, 2016 - ACS Publications
Chikungunya virus (CHIKV) is a mosquito-borne alphavirus showing a recent resurgence
and rapid spread worldwide. While vaccines are under development, there are currently no …