Design and synthesis of fungal-selective resorcylate aminopyrazole Hsp90 inhibitors

DS Huang, EV LeBlanc… - Journal of medicinal …, 2019 - ACS Publications
… of resorcylate natural products to produce fungal-selective compounds, we have … synthetic
aminopyrazole-substituted resorcylate amides with broad, potent, and fungal-selective Hsp90

Fungal-selective resorcylate aminopyrazole Hsp90 inhibitors: optimization of whole-cell anticryptococcal activity and insights into the structural origins of cryptococcal …

PT Marcyk, EV LeBlanc, DA Kuntz, A Xue… - Journal of medicinal …, 2021 - ACS Publications
… in our pursuit of fungal-selective, resorcylate inhibitors of the protein-folding chaperone
Hsp90, and building on early leads from our prior study of resorcylate aminopyrazoles (RAPs), …

Development of Fungal-selective Molecules and Strategies to Target Hsp90

EV LeBlanc - 2020 - search.proquest.com
… Ongoing efforts towards obtaining co-crystals with our novel resorcylate aminopyrazole
and guiding structure-based efforts in development of fungal-selective Hsp90 inhibitors. …

Species-selective targeting of fungal hsp90: design, synthesis, and evaluation of novel 4, 5-diarylisoxazole derivatives for the combination treatment of azole-resistant …

W Yin, T Wu, L Liu, H Jiang, Y Zhang… - Journal of Medicinal …, 2022 - ACS Publications
… (17) A recent study focusing on the Hsp90 nucleotide-binding domain (NBD) of C. albicans
… -selective Hsp90 inhibitors based on semisynthetic oxime derivatization of the resorcylate

Recent developments of HSP90 inhibitors: an updated patent review (2020-present)

J Liu, H Shu, Q Xia, Q You, L Wang - Expert Opinion on …, 2024 - Taylor & Francis
… with thiopyrazine based fungal selective HSP90 inhibitors, increasing the absorption of …
Preparation of resorcylate aminopyrazole compounds as Hsp90 inhibitors and uses thereof …

Drug design strategies for the treatment azole-resistant candidiasis

S Moghimi, M Shafiei, A Foroumadi - Expert Opinion on Drug …, 2022 - Taylor & Francis
… upstream regulators of Hsp90 function or downstream … The discovery of species-selective
Hsp90 inhibitors, which is … fungal-selective inhibition by targeting the function of Hsp90

Is the C-Terminal Domain an Effective and Selective Target for the Design of Hsp90 Inhibitors against Candida Yeast?

C Rouges, M Asad, AD Laurent, P Marchand… - Microorganisms, 2023 - mdpi.com
… Marcyk et al. published in 2021 the x-ray crystallographic structures of three fungal selective
Hsp90 inhibitors, namely resorcylate aminopyrazoles (RAPs), in complex with the nucleotide…

Pan-and isoform-specific inhibition of Hsp90: Design strategy and recent advances

J Yu, C Zhang, C Song - European Journal of Medicinal Chemistry, 2022 - Elsevier
… pan-inhibitors of Hsp90 based on the classification of binding sites and illustrated design
strategies … We summed up current isoform-specific Hsp90 inhibitors including their discovery …

Target-and prodrug-based design for fungal diseases and cancer-associated fungal infections

N Liu, J Tu, Y Huang, W Yang, Q Wang, Z Li… - Advanced Drug Delivery …, 2023 - Elsevier
… NBDs enabled the synthesis of fungal-selective Hsp90 inhibitors. … identified as a selective
Hsp90 inhibitor with an inhibitory … A series of synthetic resorcylate aminopyrazoles (RAPs) with …

Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans

C Li, J Tu, G Han, N Liu, C Sheng - European journal of medicinal chemistry, 2022 - Elsevier
… generation of Hsp90/HDAC dual inhibitors were designed as … J5 exhibited fungal-selective
inhibitory effects on Hsp90 and … due to the fungal-selective inhibition on Hsp90 and HDACs. …