New drugs for human African trypanosomiasis: a twenty first century success story

EA Dickie, F Giordani, MK Gould, P Mäser… - Tropical medicine and …, 2020 - mdpi.com
The twentieth century ended with human African trypanosomiasis (HAT) epidemics raging
across many parts of Africa. Resistance to existing drugs was emerging, and many programs …

Recent investigations into synthesis and pharmacological activities of phenoxy acetamide and its derivatives (chalcone, indole and quinoline) as possible therapeutic …

FH Al-Ostoot, Zabiulla, S Salah, SA Khanum - Journal of the Iranian …, 2021 - Springer
Medicinal chemistry can rightfully be regarded as a cornerstone in the public health of our
modern society that combines chemistry and pharmacology with the aim of designing and …

Direct and indirect targeting of HOXA9 transcription factor in acute myeloid leukemia

M Lambert, M Alioui, S Jambon, S Depauw… - Cancers, 2019 - mdpi.com
HOXA9 (Homeobox A9) is a homeotic transcription factor known for more than two decades
to be associated with leukemia. The expression of HOXA9 homeoprotein is associated with …

Novel cationic aryl bithiophene/terthiophene derivatives as corrosion inhibitors by chemical, electrochemical and surface investigations

MA Ismail, MM Shaban, E Abdel-Latif… - Scientific Reports, 2022 - nature.com
Two novel bithienyl fluorobenzamidine derivatives namely, 4-([2, 2′: 5′, 2′′-
terthiophen]-5-yl)-2-fluorobenzamidine hydrochloride salt (MA-1615), 5′-(4-amidino-3 …

HOXA9 overexpression contributes to stem cell overpopulation that drives development and growth of colorectal cancer

B Osmond, COB Facey, C Zhang… - International Journal of …, 2022 - mdpi.com
HOX proteins are transcription factors that regulate stem cell (SC) function, but their role in
the SC origin of cancer is under-studied. Aberrant expression of HOX genes occurs in many …

Biological activity of newly synthesized benzimidazole and benzothizole 2, 5-disubstituted furane derivatives

L Racané, I Zlatar, N Perin, M Cindrić, V Radovanović… - Molecules, 2021 - mdpi.com
Newly designed and synthesized cyano, amidino and acrylonitrile 2, 5-disubstituted furane
derivatives with either benzimidazole/benzothiazole nuclei have been evaluated for …

Positively selected modifications in the pore of TbAQP2 allow pentamidine to enter Trypanosoma brucei

AH Alghamdi, JC Munday, GD Campagnaro, D Gurvic… - Elife, 2020 - elifesciences.org
Mutations in the Trypanosoma brucei aquaporin AQP2 are associated with resistance to
pentamidine and melarsoprol. We show that TbAQP2 but not TbAQP3 was positively …

In Silico and In Vitro Evaluation of Some Amidine Derivatives as Hit Compounds towards Development of Inhibitors against Coronavirus Diseases

AHE Hassan, SM El-Sayed, M Yamamoto, J Gohda… - Viruses, 2023 - mdpi.com
Coronaviruses, including SARS-CoV-2, SARS-CoV, MERS-CoV and influenza A virus,
require the host proteases to mediate viral entry into cells. Rather than targeting the …

Investigation of the effect of structure modification of furamidine on the DNA minor groove binding and antiprotozoal activity

AA Farahat, A Kumar, T Wenzler, R Brun, A Paul… - European Journal of …, 2023 - Elsevier
New analogs of the antiprotozoal agent Furamidine were prepared utilizing Stille coupling
reactions and amidation of the bisnitrile intermediate using lithium bis-trimethylsilylamide …

X-ray structure characterization of the selective recognition of at base pair sequences

EN Ogbonna, A Paul, AA Farahat… - ACS bio & med …, 2023 - ACS Publications
The rational design of small molecules that target specific DNA sequences is a promising
strategy to modulate gene expression. This report focuses on a diamidinobenzimidazole …