Four Partners, Three‐Step, One‐Pot Reaction for a Library of New 2‐Alkyl(dialkyl)aminoquinazolin‐4(3<i>H</i>)‐ones

Caruso, Anna; Lancelot, Jean‐Charles; El‐Kashef, Hussein; Panno, Antonella; Sinicropi, Maria Stefania; Legay, Rémi; Lesnard, Aurélien; Lepailleur, Alban; Rault, Syl­vain

doi:10.1002/jhet.1942

Cited by 8 publications

(6 citation statements)

References 61 publications

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“…3-Aminodibenzofurans 1a-b, were used as starting materials in the synthesis of a series of new 3-(alkyl(dialkyl)amino)benzofuro [2,3-f]quinazolin-1(2H)-ones 4e17 via a one-pot three-component reaction (Scheme 1) [29,34,40]. Compound 1a was prepared, however, according to a reported method [41].…”

Section: Chemistrymentioning

confidence: 99%

3-(Dipropylamino)-5-hydroxybenzofuro[2,3-f]quinazolin-1(2H)-one (DPA-HBFQ-1) plays an inhibitory role on breast cancer cell growth and progression

Rizza

Pellegrino

Caruso

et al. 2016

European Journal of Medicinal Chemistry

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Section: Chemistrymentioning

confidence: 99%

3-(Dipropylamino)-5-hydroxybenzofuro[2,3-f]quinazolin-1(2H)-one (DPA-HBFQ-1) plays an inhibitory role on breast cancer cell growth and progression

Rizza

Pellegrino

Caruso

et al. 2016

European Journal of Medicinal Chemistry

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“…Amongst these natural compounds, the alkaloid carbazole is one of the relevant structural motifs in drug discovery. Indeed, carbazoles have been largely investigated for their various biological properties (antibacterial, anti-inflammatory, psychotropic, anti-histamine, and antitumor) [6,7,8,9,10,11,12] and also antioxidant, antiviral, and neuroprotective activities [1,2,13,14,15,16,17,18,19].…”

Section: Introductionmentioning

confidence: 99%

Carbazole Derivatives as Antiviral Agents: An Overview

et al. 2019

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Viruses represent the most common cause of infectious diseases worldwide and those with rapid propagation and high infection rates cause human and animal pandemics. These fast-spreading diseases are generally treated with antiviral drugs but, often, drug resistance occurs because of the ability of the pathogens to mutate rapidly and become less susceptible to the treatments. Even though new antivirals have been approved, e.g., in HIV (human immunodeficiency virus) and HCV (hepatitis C virus) therapeutic areas, the need to dispose of new pharmaceutical tools for the management of infections that still have no treatment is of growing interest. In these areas, carbazole represents an important privileged scaffold in drug discovery. Many compounds with a carbazolic core have been developed and some of them have shown antiviral activity. This review provides an overview on some already known carbazole derivatives, pointing the attention on the running progresses in identifying new molecules with carbazolic structure, that have shown interesting and encouraging in vitro and in vivo properties. These drugs may be exploited as valid alternatives in antiviral therapy.

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“…In particular, carbazoles closely related to previously studied indole derivatives [9][10][11][12][13][14][15][16], represent an important and heterogeneous class of anticancer agents [17][18][19], used also for other many biological properties [20]. The activity of these compounds seems to be related to different mechanisms of action including the ability to act as DNA intercalating agents and interfere with specific DNA-dependent enzymes, such as topoisomerases and telomerase, or inhibit other proteins such as cyclin-dependent kinases and estrogen receptors [21][22][23][24][25][26].…”

Section: Introductionmentioning

confidence: 99%

“…Fig. (5).Structure and activity of pyrrolo[2,3-a]carbazole derivatives(14)(15)(16)(17)(18). IC 50 values are the concentrations for 50% inhibition of Pim Kinases.…”

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Carbazole Derivatives as Kinase-Targeting Inhibitors for Cancer Treatment

Ceramella

Iacopetta

Barbarossa

et al. 2020

MRMC

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Protein Kinases (PKs) are a heterogeneous family of enzymes that modulate several biological pathways, including cell division, cytoskeletal rearrangement, differentiation and apoptosis. In particular, due to their crucial role during human tumorigenesis and cancer progression, PKs are ideal targets for the design and development of effective and low toxic chemotherapeutics and represent the second group of drug targets after G-protein-coupled receptors. Nowadays, several compounds have been claimed to be PKs inhibitors, and some of them, such as imatinib, erlotinib and gefitinib, have already been approved for clinical use, whereas more than 30 others are in various phases of clinical trials. Among them, some natural or synthetic carbazole-based molecules represent promising PKs inhibitors due to their capability to interfere with PK activity by different mechanisms of action including the ability to act as DNA intercalating agents, interfere with the activity of enzymes involved in DNA duplication, such as topoisomerases and telomerases, and inhibit other proteins such as cyclindependent kinases or antagonize estrogen receptors. Thus, carbazoles can be considered a promising this class of compounds to be adopted in targeted therapy of different types of cancer.

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Four Partners, Three‐Step, One‐Pot Reaction for a Library of New 2‐Alkyl(dialkyl)aminoquinazolin‐4(3H)‐ones

Cited by 8 publications

References 61 publications

3-(Dipropylamino)-5-hydroxybenzofuro[2,3-f]quinazolin-1(2H)-one (DPA-HBFQ-1) plays an inhibitory role on breast cancer cell growth and progression

3-(Dipropylamino)-5-hydroxybenzofuro[2,3-f]quinazolin-1(2H)-one (DPA-HBFQ-1) plays an inhibitory role on breast cancer cell growth and progression

Carbazole Derivatives as Antiviral Agents: An Overview

Carbazole Derivatives as Kinase-Targeting Inhibitors for Cancer Treatment

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