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List of works by Vincent C Njar

17alpha-Hydroxylase/17,20 lyase inhibitor VN/124-1 inhibits growth of androgen-independent prostate cancer cells via induction of the endoplasmic reticulum stress response.

scientific article

2-Methoxycanthin-6-one: A New Alkaloid from the Stem Wood of Quassia amara

scientific article published in June 1993

20-amino and 20,21-aziridinyl pregnene steroids: development of potent inhibitors of 17 alpha-hydroxylase/C17,20-lyase (P450 17)

scientific article published on 01 September 1996

4-Pregnen-21-ol-3,20-dione-21-(4-bromobenzenesulfonate) (NSC 88915) and related novel steroid derivatives as tyrosyl-DNA phosphodiesterase (Tdp1) inhibitors

scientific article

A new simple and high-yield synthesis of 5α-dihydrotestosterone (DHT), a potent androgen receptor agonist.

scientific article published on 05 October 2012

A new simple and high-yield synthesis of suberoylanilide hydroxamic acid and its inhibitory effect alone or in combination with retinoids on proliferation of human prostate cancer cells

scientific article published on July 2005

Androgen receptor inactivation contributes to antitumor efficacy of 17{alpha}-hydroxylase/17,20-lyase inhibitor 3beta-hydroxy-17-(1H-benzimidazole-1-yl)androsta-5,16-diene in prostate cancer.

scientific article published on August 2008

Anti-tumor effects of a novel retinoic acid metabolism blocking agent VN/14-1 in the N-methyl-N-nitrosourea-induced rat mammary carcinoma model and its effects on the uterus

scientific article

Antifertility activity of Quassia amara: quassin inhibits the steroidogenesis in rat Leydig cells in vitro

scientific article published on April 1995

Aromatase inhibitors and breast cancer

scientific article published on 01 August 1996

Aromatase inhibitors and their application in breast cancer treatment*.

scientific article

Aromatase inhibitors in advanced breast cancer: mechanism of action and clinical implications

scientific article published on 01 July 1998

Autophagy inhibition synergistically enhances anticancer efficacy of RAMBA, VN/12-1 in SKBR-3 cells, and tumor xenografts

scientific article published on 14 February 2012

Biochemical assessment of limits to estrogen synthesis in porcine follicles

scientific article published on 2 April 2003

Biotransformation of progesterone to 14 alpha-hydroxypregna-1,4-diene-3,20-dione, a novel fungal metabolite, by Colletotrichum antirrhini.

scientific article published on March 1985

CYP17 inhibitors for prostate cancer therapy

scientific article

CYP17 inhibitors for prostate cancer treatment--an update.

scientific article published on January 2008

Competitive antagonism between the nicotinic allosteric potentiating ligand galantamine and kynurenic acid at alpha7* nicotinic receptors.

scientific article

Comprehensive pharmacology and clinical efficacy of aromatase inhibitors

scientific article

Concerning the pathway from 19-oxoandrost-4-ene-3,17-dione to estrone

scientific article published on October 1987

Cytochrome P450c17-expressing Escherichia coli as a first-step screening system for 17alpha-hydroxylase-C17,20-lyase inhibitors

scientific article published on 01 February 1999

Cytochrome p450 retinoic acid 4-hydroxylase inhibitors: potential agents for cancer therapy

scientific article

Design, synthesis, and evaluation of novel mutual prodrugs (hybrid drugs) of all-trans-retinoic acid and histone deacetylase inhibitors with enhanced anticancer activities in breast and prostate cancer cells in vitro.

scientific article

Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer.

scientific article published on 28 January 2015

Dissecting major signaling pathways in prostate cancer development and progression: Mechanisms and novel therapeutic targets

scientific article

Effects of new 17alpha-hydroxylase/C(17,20)-lyase inhibitors on LNCaP prostate cancer cell growth in vitro and in vivo

scientific article published on October 1999

Effects of novel 17-azolyl compounds on androgen synthesis in vitro and in vivo

scientific article published on 01 December 1999

Effects of novel retinoic acid metabolism blocking agent (VN/14-1) on letrozole-insensitive breast cancer cells.

scientific article published on December 2006

Evaluation of 6,7-aziridinyl steroids and related compounds as inhibitors of aromatase (P-450arom)

scientific article published on 01 January 1995

First MNKs degrading agents block phosphorylation of eIF4E, induce apoptosis, inhibit cell growth, migration and invasion in triple negative and Her2-overexpressing breast cancer cell lines

scientific article published on January 2014

First chemical feature-based pharmacophore modeling of potent retinoidal retinoic acid metabolism blocking agents (RAMBAs): identification of novel RAMBA scaffolds.

scientific article published on 17 November 2011

First pharmacophore-based identification of androgen receptor down-regulating agents: discovery of potent anti-prostate cancer agents.

scientific article

Galeterone and The Next Generation Galeterone Analogs, VNPP414 and VNPP433-3β Exert Potent Therapeutic Effects in Castration-/Drug-Resistant Prostate Cancer Preclinical Models In Vitro and In Vivo

scientific article published on 24 October 2019

Galeterone and VNPT55 disrupt Mnk-eIF4E to inhibit prostate cancer cell migration and invasion

scientific article published on 12 September 2016

Galeterone and VNPT55 induce proteasomal degradation of AR/AR-V7, induce significant apoptosis via cytochrome c release and suppress growth of castration resistant prostate cancer xenografts in vivo.

scientific article

Galeterone and its analogs inhibit Mnk-eIF4E axis, synergize with gemcitabine, impede pancreatic cancer cell migration, invasion and proliferation and inhibit tumor growth in mice

scientific article published on 24 December 2016

Guidelines for the use and interpretation of assays for monitoring autophagy (3rd edition)

scientific article

Identification of Novel Steroidal Androgen Receptor Degrading Agents Inspired by Galeterone 3β-Imidazole Carbamate

scientific article published on 23 May 2016

Improved synthesis of histone deacetylase inhibitors (HDIs) (MS-275 and CI-994) and inhibitory effects of HDIs alone or in combination with RAMBAs or retinoids on growth of human LNCaP prostate cancer cells and tumor xenografts

scientific article published on 8 December 2007

Inhibitors of 17alpha-hydroxylase/17,20-lyase (CYP17): potential agents for the treatment of prostate cancer

scientific article

Inhibitory effects of retinoic acid metabolism blocking agents (RAMBAs) on the growth of human prostate cancer cells and LNCaP prostate tumour xenografts in SCID mice.

scientific article published on February 2006

Letter to the editor

scientific article published on 25 July 2016

MS-275 synergistically enhances the growth inhibitory effects of RAMBA VN/66-1 in hormone-insensitive PC-3 prostate cancer cells and tumours.

scientific article published on 18 March 2008

Mechanistic studies on aromatase and related C-C bond cleaving P-450 enzymes

scientific article

Methyl angolensate: the antiulcer agent of the stem bark of Entandrophragma angolense

scientific article published on 01 February 1995

Murine toxicology and pharmacokinetics evaluation of retinoic acid metabolism blocking agent (RAMBA), VN/12-1.

scientific article published on 13 May 2012

Murine toxicology and pharmacokinetics of novel retinoic acid metabolism blocking agents

scientific article published on 08 March 2007

New insights into the androgen-targeted therapies and epigenetic therapies in prostate cancer.

scientific article published on 12 October 2011

Novel 17-azolyl steroids, potent inhibitors of human cytochrome 17 alpha-hydroxylase-C17,20-lyase (P450(17) alpha): potential agents for the treatment of prostate cancer.

scientific article

Novel 19-(cyclopropylamino)-androst-4-en-3,17-dione: a mechanism-based inhibitor of aromatase

scientific article published on 01 January 1996

Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model

scientific article

Novel C-4 heteroaryl 13-cis-retinamide Mnk/AR degrading agents inhibit cell proliferation and migration and induce apoptosis in human breast and prostate cancer cells and suppress growth of MDA-MB-231 human breast and CWR22Rv1 human prostate tumor x

scientific article published on 12 February 2015

Novel galeterone analogs act independently of AR and AR-V7 for the activation of the unfolded protein response and induction of apoptosis in the CWR22Rv1 prostate cancer cell model.

scientific article published in August 2017

Novel retinoic acid metabolism blocking agents endowed with multiple biological activities are efficient growth inhibitors of human breast and prostate cancer cells in vitro and a human breast tumor xenograft in nude mice

scientific article published in December 2004

Novel retinoic acid metabolism blocking agents have potent inhibitory activities on human breast cancer cells and tumour growth.

scientific article

Novel, potent anti-androgens of therapeutic potential: recent advances and promising developments.

scientific article published on April 2010

Pharmacokinetic profile of 3beta-hydroxy-17-(1H-1,2,3-triazol-1-yl)androsta-5,16-diene (VN/87-1), a potent androgen synthesis inhibitor, in mice.

scientific article

Pharmacokinetics of novel inhibitors of androgen synthesis after intravenous administration in mice.

scientific article published on 25 April 2003

Potent CYP17 inhibitors: improved syntheses, pharmacokinetics and anti-tumor activity in the LNCaP human prostate cancer model.

scientific article published in October 2004

Potent anti-prostate cancer agents derived from a novel androgen receptor down-regulating agent.

scientific article

Potent inhibition of retinoic acid metabolism enzyme(s) by novel azolyl retinoids

scientific article published on 01 September 2000

Pregnenolone stimulates LNCaP prostate cancer cell growth via the mutated androgen receptor.

scientific article

Prolonging hormone sensitivity in prostate cancer xenografts through dual inhibition of AR and mTOR.

scientific article

Promise and challenges in drug discovery and development of hybrid anticancer drugs

scientific article published on 01 November 2009

Prospects for Clinical Development of Stat5 Inhibitor IST5-002: High Transcriptomic Specificity in Prostate Cancer and Low Toxicity In Vivo

scientific article published on 18 November 2020

Quantification of a novel retinoic acid metabolism inhibitor, 4-(1H-imidazol-1-yl)retinoic acid (VN/14-1RA) and other retinoids in rat plasma by liquid chromatography with diode-array detection

scientific article published in October 2004

Regulation of androgen receptor activity by tyrosine phosphorylation.

scientific article published on October 2006

Regulation of microsomal P450, redox partner proteins, and steroidogenesis in the developing testes of the neonatal pig.

scientific article published in September 2002

Retinoic acid metabolism blocking agents (RAMBAs) for treatment of cancer and dermatological diseases.

scientific article

Retinoids in clinical use.

scientific article published on July 2006

Simultaneous targeting of androgen receptor (AR) and MAPK-interacting kinases (MNKs) by novel retinamides inhibits growth of human prostate cancer cell lines

scientific article

Structure-Based Screen Identifies a Potent Small Molecule Inhibitor of Stat5a/b with Therapeutic Potential for Prostate Cancer and Chronic Myeloid Leukemia.

scientific article published on 29 May 2015

Synergistic effect of a novel antiandrogen, VN/124-1, and signal transduction inhibitors in prostate cancer progression to hormone independence in vitro.

scientific article published on January 2008

Synthesis and biological evaluations of putative metabolically stable analogs of VN/124-1 (TOK-001): head to head anti-tumor efficacy evaluation of VN/124-1 (TOK-001) and abiraterone in LAPC-4 human prostate cancer xenograft model

scientific article

Synthesis and evaluation of novel 17-indazole androstene derivatives designed as CYP17 inhibitors.

scientific article published on 15 August 2007

Synthesis of 10 beta-(1'-azirinyl)estr-4-en-3,17-dione as an aromatase inhibitor

scientific article published on 01 March 1996

Synthesis of [16,16,19(-2)H3; 19(-3)H]19-oxo-androst-4-ene-3,17-dione

scientific article published on 01 May 1988

Synthesis of c-2, 3, 17 and 19-oxygenated androgens

scientific article published on March 1988

Synthesis of novel 21-trifluoropregnane steroids: inhibitors of 17 alpha-hydroxylase/17,20-lyase (17 alpha-lyase)

scientific article published on 01 June 1997

Synthesis of novel C17 steroidal carbamates. Studies on CYP17 action, androgen receptor binding and function, and prostate cancer cell growth

scientific article

Systematic structure modifications of multitarget prostate cancer drug candidate galeterone to produce novel androgen receptor down-regulating agents as an approach to treatment of advanced prostate cancer

scientific article

Targeting cytochrome P450 enzymes: a new approach in anti-cancer drug development

scientific article

Targeting drug-metabolizing enzymes for effective chemoprevention and chemotherapy.

scientific article

Targeting of protein translation as a new treatment paradigm for prostate cancer

scientific article published on 9 March 2017

The Coffey Lecture: steroidogenic enzyme inhibitors and hormone dependent cancer

scientific article

The combination of the histone deacetylase inhibitor vorinostat and synthetic triterpenoids reduces tumorigenesis in mouse models of cancer

scientific article

The retinamide VNLG-152 inhibits f-AR/AR-V7 and MNK-eIF4E signaling pathways to suppress EMT and castration-resistant prostate cancer xenograft growth.

scientific article published on 11 January 2018

Three dimensional pharmacophore modeling of human CYP17 inhibitors. Potential agents for prostate cancer therapy.

scientific article published in June 2003

VN/14-1 induces ER stress and autophagy in HP-LTLC human breast cancer cells and has excellent oral pharmacokinetic profile in female Sprague Dawley rats

scientific article

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