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Literature DB >> 21561408

Synthesis and cytotoxic activity of new β-carboline derivatives.

A Peduto¹, V More, P de Caprariis, M Festa, A Capasso, S Piacente, L De Martino, V De Feo, R Filosa.

Abstract

On the basis of harmine and 1-methoxy-canthin-6-one chemical structures, a series of novel 1,4-disubstituted and 1,4,9-trisubstituted β-carbolines and tetracyclic derivatives were designed and synthesized. Cytotoxic activities of these compounds in vitro were investigated in a human tumor cell line panel. Almost all compounds demonstrated interesting cytotoxic activities in particular against prostate cancer cells PC-3 with IC50 in the low micromolar range. Compound X was found to be the most potent one with IC50 value of 8.0 µM; this suggests further studies with models of prostate cancer.

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Year: 2011 PMID： 21561408 DOI： 10.2174/138955711795843383

Source DB: PubMed Journal: Mini Rev Med Chem ISSN： 1389-5575 Impact factor: 3.862

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Cited

8 in total

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Journal: J Biomol Screen Date: 2014-03-05

2. The 1,4 benzoquinone-featured 5-lipoxygenase inhibitor RF-Id induces apoptotic death through downregulation of IAPs in human glioblastoma cells.

Authors: S Zappavigna; M Scuotto; A M Cossu; D Ingrosso; M De Rosa; C Schiraldi; R Filosa; M Caraglia
Journal: J Exp Clin Cancer Res Date: 2016-10-22

3. Discovery of novel phthalimide analogs: Synthesis, antimicrobial and antitubercular screening with molecular docking studies.

Authors: Heba S Rateb; Hany E A Ahmed; Sahar Ahmed; Saleh Ihmaid; Tarek H Afifi
Journal: EXCLI J Date: 2016-12-06 Impact factor: 4.068

4. Introducing novel potent anticancer agents of 1H-benzo[f]chromene scaffolds, targeting c-Src kinase enzyme with MDA-MB-231 cell line anti-invasion effect.

Authors: Hany E A Ahmed; Mohammed A A El-Nassag; Ahmed H Hassan; Rawda M Okasha; Saleh Ihmaid; Ahmed M Fouda; Tarek H Afifi; Ateyatallah Aljuhani; Ahmed M El-Agrody
Journal: J Enzyme Inhib Med Chem Date: 2018-12 Impact factor: 5.051

5. A Hydroquinone-Based Derivative Elicits Apoptosis and Autophagy via Activating a ROS-Dependent Unfolded Protein Response in Human Glioblastoma.

Authors: Silvia Zappavigna; Alessia Maria Cossu; Marianna Abate; Gabriella Misso; Angela Lombardi; Michele Caraglia; Rosanna Filosa
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Synthesis and cytotoxic activity of new β-carboline derivatives.

1. Enzymatic Characterization of ER Stress-Dependent Kinase, PERK, and Development of a High-Throughput Assay for Identification of PERK Inhibitors.

2. The 1,4 benzoquinone-featured 5-lipoxygenase inhibitor RF-Id induces apoptotic death through downregulation of IAPs in human glioblastoma cells.

3. Discovery of novel phthalimide analogs: Synthesis, antimicrobial and antitubercular screening with molecular docking studies.

4. Introducing novel potent anticancer agents of 1H-benzo[f]chromene scaffolds, targeting c-Src kinase enzyme with MDA-MB-231 cell line anti-invasion effect.

5. A Hydroquinone-Based Derivative Elicits Apoptosis and Autophagy via Activating a ROS-Dependent Unfolded Protein Response in Human Glioblastoma.

Review 6. Structures and Biological Activities of Alkaloids Produced by Mushrooms, a Fungal Subgroup.

7. A new route to α-carbolines based on 6π-electrocyclization of indole-3-alkenyl oximes.

8. Binding of Harmine Derivatives to DNA: A Spectroscopic Investigation.