Biosynthetic Derivatization of Antimicrobial Orthosomycins to Engage a Unique Ribosomal Binding Site

AE Yñigez-Gutierrez - 2021 - ir.vanderbilt.edu
… to related ansamycin scaffolds.The first total synthesis of an … illustrated that the hydroquinone
form of geldanamycin was as … for in vitro analysis; however, a low-micromolar affinity was …

Synthesis and characterization of 64Cu-labeled Geldanamycin derivative for imaging HSP90 expression in breast cancer

F Li, Y Fan, L Zhou, DR Martin, Z Liu, Z Li - Nuclear Medicine and Biology, 2024 - Elsevier
vivo instability limit the use of GM as an anticancer drug or diagnostic ligand in clinical trials.
As a member of the ansamycin … cells, we assessed the cellular binding affinity of [ 64 Cu]Cu-…

Bacteria as a treasure house of secondary metabolites with anticancer potential

CD Mohan, S Rangappa, SC Nayak… - Seminars in cancer …, 2022 - Elsevier
… take place in middle- or low-income countries. The leading … ring along with quinine-hydroquinone
and one of the rings … cisplatin) towards a wide range of cancer cell lines and in vivo

[HTML][HTML] Inhibitors of the Plasmodium falciparum Hsp90 towards Selective Antimalarial Drug Design: The Past, Present and Future

ML Stofberg, C Caillet, M de Villiers, T Zininga - Cells, 2021 - mdpi.com
… Geldanamycin (GA), a benzoquinone ansamycin compound … , such as low toxicity profiles
and increased in vivo activity and … differences between the 17-DMAG binding affinities for …

Design, synthesis and antitumor efficacy evaluation of a series of novel β-elemene-based macrocycles

X Qi, S Jiang, Z Hui, Y Gao, Y Ye, F Lirussi… - Bioorganic & Medicinal …, 2022 - Elsevier
… They often display high-affinity binding, and are able to … conformations restrictions have
lower entropy loss when … fragments affect their antitumor activity in vitro, we also found that rings …

[PDF][PDF] Inhibitors of the Plasmodium falciparum Hsp90 towards Selective Antimalarial Drug Design: The Past, Present and Future. Cells 2021, 10, 2849

ML Stofberg, C Caillet, M de Villiers, T Zininga - 2021 - academia.edu
… Geldanamycin (GA), a benzoquinone ansamycin compound … , such as low toxicity profiles
and increased in vivo activity and … differences between the 17-DMAG binding affinities for …

[图书][B] Small Molecule Modulation of the Hsp90 Proteostasis Network for Neuropathic Protection

BM Keegan - 2023 - search.proquest.com
… compounds that exhibit increased efficacy and potency toward … manifests T200Yfold higher
affinity for ATP than the … these heteroprotein complexes and their differential binding affinities. …

p-Benzoquinone as a privileged scaffold of pharmacological significance: A Review

P Silakari, P Piplani - Mini reviews in medicinal chemistry, 2020 - ingentaconnect.com
… was used for the oxidation of hydroquinone dimethyl ether (9) to … antioxidant action in AD
both in vitro [47] and in vivo [48] … Geldanamycin (16) was the first ansamycin antibiotic found in …

[HTML][HTML] An update on the status of HSP90 inhibitors in cancer clinical trials

S Rastogi, A Joshi, N Sato, S Lee, JB Trepel… - Cell Stress and …, 2024 - Elsevier
… GA was a first generation ansamycin analog with a … of 17-AAG, a highly soluble hydroquinone
hydrochloride IPI-504 (… While it exhibited similar antitumor activity as GA in vitro, in vivo

[HTML][HTML] Inhibitors of HSP90 in melanoma

A Mielczarek-Lewandowska, ML Hartman, M Czyz - Apoptosis, 2020 - Springer
… Cell sensitivity to ansamycin inhibitors of HSP90 was also … This could result from similar
affinity of quinone and hydroquinone … cell apoptosis and inhibit melanoma tumor growth in vivo […