Synthetic approaches, anticancer potential, HSP90 inhibition, multitarget evaluation, molecular modeling and apoptosis mechanistic study of thioquinazolinone …

HW El-Shafey, RM Gomaa, SM El-Messery… - Bioorganic Chemistry, 2020 - Elsevier
New series of compounds bearing 2-thioquinazolinone scaffold were designed, synthesized
as HSP90 inhibitors. Anti-proliferative activity of the synthesized compounds was evaluated …

Quinazoline based HSP90 inhibitors: synthesis, modeling study and ADME calculations towards breast cancer targeting

HW El-Shafey, RM Gomaa, SM El-Messery… - Bioorganic & Medicinal …, 2020 - Elsevier
A new 2-thioquinazolinones series was designed and synthesized as HSP90 inhibitors
based on the structure of hit compound VII obtained by virtual screening approach. Their in …

Cucurbitacin D is a disruptor of the HSP90 chaperone machinery

JA Hall, S Seedarala, N Rice, L Kopel… - Journal of natural …, 2015 - ACS Publications
Heat shock protein 90 (Hsp90) facilitates the maturation of many newly synthesized and
unfolded proteins (clients) via the Hsp90 chaperone cycle, in which Hsp90 forms a …

Hsp90 inhibitors sensitise human colon cancer cells to topoisomerase I poisons by depletion of key anti-apoptotic and cell cycle checkpoint proteins

AV McNamara, M Barclay, AJM Watson… - Biochemical …, 2012 - Elsevier
Hsp90 and topoisomerase I are both targets for chemotherapeutic agents. Topoisomerase I
poisons are standard clinical treatments, whilst Hsp90 inhibitors are progressing through …

[PDF][PDF] A novel, improved throughput bioassay for determining the delative speed of antimalarial drug action using fluorescent vitality probes

D Laming - 2020 - commons.ru.ac.za
Malaria is one of the most prevalent diseases in Africa and Plasmodium falciparum is widely
accepted as the most virulent of the malaria parasite species, with a fatality rate of 15–20 …

Der Einfluss von Chemotherapeutika mit Hypoxie-induzierbarer Faktor (HIF)-modulierendem Potential sowie eines Verlustes des HIF-Regulators von Hippel-Lindau …

S Trojandt - 2015 - openscience.ub.uni-mainz.de
Der Transkriptionsfaktor Hypoxie-induzierbarer Faktor (HIF) gibt dem Organismus die
Möglichkeit, sich auf zellulärer Ebene an unterschiedliche Sauerstoffverhältnisse …