Nonsteroidal Androgen Receptor Ligands: Versatile Syntheses and Biological Data

Varchi, Greta; Guerrini, Andrea; Tesei, Anna; Brigliadori, Giovanni; Bertucci, Carlo; Donato, Marzia Di; Castoria, Gabriella

doi:10.1021/ml3000269

Cited by 11 publications

(9 citation statements)

References 28 publications

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“…Efforts to target androgen receptor signaling have largely focused on decreasing circulating androgens (CYP17 inhibition) or blocking the binding of androgens to their cognate receptor (AR inhibition) (13)(14)(15)(16)(17). Production of androgens is dependent upon the activity of cytochrome P450 17α-hydroxylase/17,20lyase (CYP17 lyase) (18).…”

Section: Introductionmentioning

confidence: 99%

Seviteronel, a Novel CYP17 Lyase Inhibitor and Androgen Receptor Antagonist, Radiosensitizes AR-Positive Triple Negative Breast Cancer Cells

et al. 2020

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Michmerhuizen et al. Seviteronel Radiosensitizes AR+ TNBC RT, suggesting that seviteronel may have a different mechanism of radiosensitization compared to other AR inhibitors. Enzalutamide and seviteronel treatment also had different effects on AR and AR target genes as measured by immunoblot and qPCR. These results implicate AR as a mediator of radioresistance in AR+ TNBC models and support the use of seviteronel as a radiosensitizing agent in AR+ TNBC.

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Section: Introductionmentioning

confidence: 99%

Seviteronel, a Novel CYP17 Lyase Inhibitor and Androgen Receptor Antagonist, Radiosensitizes AR-Positive Triple Negative Breast Cancer Cells

et al. 2020

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“…[29] On the other hand (B), aza-Darzens-type condensations between carbenoid reagents and N-tert-butanesulfinyl imines have been disclosed with a rather large array of carbanions. These include: lithiated halomethylphosphonates like 14, [30] zincated propargylic and allylic bromides 15 [31] and 16, [32] a lithiated (chloroethyl)oxazoline, [33] lithiated bromoesters such as 17, [34] lithiated halomethanes 18 and 19, [35] the sodium anions of bromoform, [36] chloroform [14] and halo methylsulfones (i.e. 20), [37] and the lithium or potassium anions of dihalo methanes (21).…”

Section: N-acylation Of Tert-butanesulfinamidesmentioning

confidence: 99%

tert-Butanesulfinamides as Nitrogen Nucleophiles in Carbon–Nitrogen Bond Forming Reactions

Hernandez

Chemla

Ferreira

et al. 2016

Chimia

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The use of tert-butanesulfinamides as nitrogen nucleophiles in carbon-nitrogen bond forming reactions is reviewed. This field has grown in the shadow of the general interest in N-tert-butanesulfinyl imines for asymmetric synthesis and occupies now an important place in its own right in the chemistry of the chiral amine reagent tert-butanesulfinamide. This article provides an overview of the area and emphasizes recent contributions wherein the tert-butanesulfinamides act as chiral auxiliaries or perform as nitrogen donors in metal-catalyzed amination reactions.

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“…HRPC implies that the cancer no longer responds to hormone therapy, but the fact that prostate cancer responds to drugs like abiraterone and MDV 3100 shows that the tumor is still "hormone sensitive". 29 Various steroidal AR ligands have been developed, but their use has been limited because of the poor oral bio-availability and a lack of selectivity between anabolic and androgenic effects, leading to a risk of serious side effects. The goal of immunotherapy is to stimulate the body's natural defenses in a specific manner so that they attack and destroy, or at least prevent, the proliferation of cancer cells.…”

Section: Senthamaraikannanmentioning

confidence: 99%

Recent discoveries and developments of androgen receptor based therapy for prostate cancer

Elancheran

Maruthanila²,

Ramanathan

et al. 2015

Med. Chem. Commun.

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The main focus of this review is to discuss the discoveries and developments of various therapies for prostate cancer. The AR has played an important role in prostate cancer growth and functions. This review discusses several groups of drugs that have sparingly good anti-cancer activities, as well as a similar structure and behaviour. A recent new-generation AR antagonist, Enzalutamide (MDV3100), has been approved for the treatment of advanced/metastatic prostate cancer. Nonsteroidal antiandrogens represent an important class of molecules acting as either antagonists or agonists. Recently, many therapeutic agents for prostate cancer that target the androgen receptor and reduce prostate tumour growth have been approved. The strong response to this new use of Enzalutamide provides a viable, less toxic alternative to chemotherapy.The current status of prostate cancer drugs are discussed here, but it is evident that considerably more work is needed for improvements in respect to efficacy, reduction of the side effects and treatment strategies.Med. Chem. Commun. This journal is . He carried out some postdoctoral work in the Second Shanghai Medical University, P.R. China. He is currently working in the fields of traditional knowledge-based drug design, development and delivery systems for cancer, diabetes and metabolic syndrome. MedChemCommReview

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Nonsteroidal Androgen Receptor Ligands: Versatile Syntheses and Biological Data

Cited by 11 publications

References 28 publications

Seviteronel, a Novel CYP17 Lyase Inhibitor and Androgen Receptor Antagonist, Radiosensitizes AR-Positive Triple Negative Breast Cancer Cells

Seviteronel, a Novel CYP17 Lyase Inhibitor and Androgen Receptor Antagonist, Radiosensitizes AR-Positive Triple Negative Breast Cancer Cells

tert-Butanesulfinamides as Nitrogen Nucleophiles in Carbon–Nitrogen Bond Forming Reactions

Recent discoveries and developments of androgen receptor based therapy for prostate cancer

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