Insights into amentoflavone: a natural multifunctional biflavonoid

X Xiong, N Tang, X Lai, J Zhang, W Wen, X Li… - Frontiers in …, 2021 - frontiersin.org
Amentoflavone is an active phenolic compound isolated from Selaginella tamariscina over
40 years. Amentoflavone has been extensively recorded as a molecule which displays …

Strecker reaction and α-amino nitriles: Recent advances in their chemistry, synthesis, and biological properties

VV Kouznetsov, CEP Galvis - Tetrahedron, 2018 - Elsevier
Abstract α-Amino nitrile compounds have a profound impact on bio-chemical sciences, as
they have been prepared from inexpensive starting materials and have become valuable …

Discovery of new pyrimidine-5-carbonitrile derivatives as anticancer agents targeting EGFR WT and EGFR T790M

AA Nasser, IH Eissa, MR Oun, MA El-Zahabi… - Organic & …, 2020 - pubs.rsc.org
A new series of pyrimidine-5-carbonitrile derivatives has been designed as ATP mimicking
tyrosine kinase inhibitors of the epidermal growth factor receptor (EGFR). These compounds …

Cathepsin B: Active site mapping with peptidic substrates and inhibitors

J Schmitz, E Gilberg, R Löser, J Bajorath… - Bioorganic & medicinal …, 2019 - Elsevier
The potential of papain-like cysteine proteases, such as cathepsin B, as drug discovery
targets for systemic human diseases has prevailed over the past years. The development of …

Discovery of potent, reversible, and competitive cruzain inhibitors with trypanocidal activity: a structure-based drug design approach

ML de Souza… - Journal of Chemical …, 2019 - ACS Publications
A virtual screening conducted with nearly 4 000 000 compounds from lead-like and fragment-
like subsets enabled the identification of a small-molecule inhibitor (1) of the Trypanosoma …

Structure-based discovery of novel cruzain inhibitors with distinct trypanocidal activity profiles

VC Santos, PG Leite, LH Santos, PG Pascutti… - European Journal of …, 2023 - Elsevier
Over 110 years after the first formal description of Chagas disease, the trypanocidal drugs
thus far available have limited efficacy and several side effects. This encourages the search …

Mandelic acid catalyzed one-pot three-component synthesis of α-aminonitriles and α-aminophosphonates under solvent-free conditions at room temperature

G Kaur, M Shamim, V Bhardwaj, VK Gupta… - Synthetic …, 2020 - Taylor & Francis
A simple, mild, straightforward, efficient and eco-friendly protocol has been developed for
the synthesis of a series of α-aminonitriles via the one-pot three-component Strecker …

Experimental study and computational modelling of cruzain cysteine protease inhibition by dipeptidyl nitriles

AM Dos Santos, L Cianni, D De Vita, F Rosini… - Physical Chemistry …, 2018 - pubs.rsc.org
Chagas disease affects millions of people in Latin America. This disease is caused by the
protozoan parasite Trypanossoma cruzi. The cysteine protease cruzain is a key enzyme for …

Quantum computational investigations and molecular docking studies on amentoflavone

MM Marinho, FWQ Almeida-Neto, EM Marinho… - Heliyon, 2021 - cell.com
Chagas disease is a neglected tropical disease caused by the protozoan parasite
Trypanosoma cruzi, with approximately 6–7 million people infected worldwide, becoming a …

Synthesis and structure-activity relationship studies of cruzain and rhodesain inhibitors

DA Rocha, EB Silva, IS Fortes, MS Lopes… - European Journal of …, 2018 - Elsevier
Abstract Chagas disease and Human African trypanosomiasis (HAT) are important public
health issues in Latin American and sub-Saharan African countries, respectively, and are …