Maria Valeria Raimondi

Research Field

Pyrrolomycins (PMs) are a family of naturally occurring antibiotic agents, isolated from the fermentation broth of Actinosporangium and Streptomyces species. Pursuing our studies on pyrrolomycins, we performed the total synthesis of the F-series pyrrolomycins (1-4) by microwave-assisted synthesis (MAOS), thus obtaining the title compounds in excellent yields (63-69%). Considering that there is no evidence so far of the anticancer effect of this class of compounds, we investigated PMs for their antiproliferative activity against HCT116 and MCF-7 cancer cell lines. PMs showed anticancer activity at submicromolar level with a minimal effect on normal epithelial cell line (hTERT RPE-1), and they were able to induce several morphological changes including elongated cells, cytoplasm vacuolization, long and thin filopodia as well as the appearance of tunneling nanotubes (TNTs). These data suggest that PMs could act by impairing the cell membranes and the cytoskeleton organization, with subsequent increase of ROS generation and the activation of different forms of non-apoptotic cell death.

Vacuolization

Mechanism of Action

10.1016/j.ejmech.2023.115339

Cite

Citations (3)

Synthesis, antiproliferative activity and possible mechanism of action of novel 2-acetamidobenzamides bearing the 2-phenoxy functionality

Bioorganic & Medicinal Chemistry (2015)

Demetrio Raffa Benedetta Maggio Fabiana Plescia Stella Cascioferro Maria Valeria Raimondi

Chronic myelogenous leukemia

K562 cells

Mechanism of Action

10.1016/j.bmc.2015.08.027

Cite

Citations (13)

Synthesis and antirpoliferative activity of isoxazolo[3,4-d]pyridazin-7(6H)-one derivatives

Giuseppe Daidone Benedetta Maggio Demetrio Raffa Marianna Lauricella Fabiana Plescia

Source

Cite

Citations (0)

Non-Classical Transformation of Benzendiazonium Hydrogen Sulfates. Access to 1,3-Dimethylisochromeno[4,3-c]pyrazol-5(1H)-one, a Potential Benzodiazepine Receptor Ligand

Molecules (2013)

Benedetta Maggio Demetrio Raffa Maria Valeria Raimondi Giuseppe Daidone

The compound 2-((1,3-dimethyl-1H-pyrazol-5-yl)(methyl)carbamoyl)benzene-diazonium hydrogen sulfate (10) was reacted with copper sulfate and sodium chloride, in the presence of ascorbic acid as reducing agent, to afford a mixture of the chlorinated epimers 4′-chloro-2,2′,5′-trimethyl-2′,4′-dihydrospiro[isoindoline-1,3′-pyrazol]-3-one (18) and (19), the epimers 4′-hydroxy-2,2′,5′-trimethyl-2′,4′-dihydrospiro[isoindoline-1,3′-pyrazol]-3-one (20) and (21), and N-(1,3-dimethyl-1H-pyrazol-5-yl)benzamide (22). Under the foregoing conditions, diazonium salt 10 affords neither the 2-chloro-N-(1,3-dimethyl-1H-pyrazol-5-yl)-N-methylbenzamide (23) nor the tricyclic derivative 24, the classical products of the Sandmeyer and Pschorr reactions, respectively. Finally, by heating 20 at 210 °C the compound 1,3-dimethylisochromeno[4,3-c]pyrazol-5(1H)-one (24) was obtained. The transformation under the above conditions of 2-((4-chloro-3-methyl-1-phenyl- 1H-pyrazol-5-yl)(methyl)carbamoyl)benzendiazonium hydrogen sulphate (11) afforded 4′,4′-dichloro-2,5′-dimethyl-2′-phenyl-2′,4′-dihydrospiro[isoindoline-1,3′-pyrazol]-3-one (29) as the sole reaction product.

Isoindoline

Dimethyl sulfate

Sodium methoxide

10.3390/molecules181013096

Cite

Citations (2)

2-Cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: Synthesis, antiproliferative activity, and mechanism of action

European Journal of Medicinal Chemistry (2013)

Demetrio Raffa Benedetta Maggio Maria Valeria Raimondi Maria Grazia Cusimano Giandomenico Amico

Chronic myelogenous leukemia

K562 cells

Mechanism of Action

10.1016/j.ejmech.2013.04.068

Cite

Citations (8)

Synthesis, biological evaluation, and molecular docking studies of aldotetronic acid-based LpxC inhibitors

Bioorganic Chemistry (2022)

Stefan Jakob Wimmer Katharina J. Hoff Benedikt Martin Martin Grewer Laura Denni

Docking (animal)

10.1016/j.bioorg.2022.106331

Cite

Citations (5)

Pyrrolomycins as antimicrobial agents. Microwave-assisted organic synthesis and insights into their antimicrobial mechanism of action

Bioorganic & Medicinal Chemistry (2019)

Maria Valeria Raimondi Roberta Listro Maria Grazia Cusimano Mery La Franca Teresa Faddetta

Sortase A

Sortase

Mechanism of Action

Docking (animal)

IC50

Lead compound

10.1016/j.bmc.2019.01.010

Cite

Citations (41)

Sintesi di un isostero del 3,5-dimetil-6-fenil-8-(trifluorometil)-5,6-diidropirazolo[3,4-f][1,2,3,5]tetrazepin-4(3H)-one (CF3-TZP) con potenziale attività biologica

D. Raffa Fabiana Plescia Giovanna Li Petri Benedetta Maggio Maria Valeria Raimondi

Source

Cite

Citations (0)

Anthranilamide-based 2-phenylcyclopropane-1-carboxamides, 1,1'-biphenyl-4-carboxamides and 1,1'-biphenyl-2-carboxamides: Synthesis biological evaluation and mechanism of action

European Journal of Medicinal Chemistry (2017)

Demetrio Raffa Fabiana Plescia Benedetta Maggio Maria Valeria Raimondi Antonella D’Anneo

Biphenyl

Derivative (finance)

Carboxamide

K562 cells

Mechanism of Action

Mode of Action

10.1016/j.ejmech.2017.03.051

Cite

Citations (10)

Editorial: Emerging heterocycles as bioactive compounds

Frontiers in Chemistry (2023)

Giovanna Li Petri Ralph Holl Virginia Spanò Marilia Barreca Ignazio Sardo

EDITORIAL article Front. Chem., 26 April 2023Sec. Medicinal and Pharmaceutical Chemistry Volume 11 - 2023 | https://doi.org/10.3389/fchem.2023.1202192

10.3389/fchem.2023.1202192

Cite

Citations (4)

Maria Valeria Raimondi

Papers

Citation

H-Index

i-10 index

Papers

Citation

H-Index

i-10 index