Improved Procedures for Gram-Scale Synthesis of Galeterone 3β-Imidazole and Galeterone 3β-Pyridine Methoxylate, Potent Androgen Receptor/Mnk Degrading Agents-Reference-Cited by-同舟云学术

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Improved Procedures for Gram-Scale Synthesis of Galeterone 3β-Imidazole and Galeterone 3β-Pyridine Methoxylate, Potent Androgen Receptor/Mnk Degrading Agents

Published:2016-08-23 Issue:9 Volume:20 Page:1654-1661
ISSN:1083-6160
Container-title:Organic Process Research & Development
language:en
Short-container-title:Org. Process Res. Dev.

Author:

Purushottamachar Puranik¹,Murigi Francis N.¹,Njar Vincent C. O.¹

Affiliation:

1. Department of Pharmacology, ‡Center for Biomolecular Therapeutics, and §Marlene and Stewart Greenebaum Comprehensive Cancer Center, University of Maryland School of Medicine, 685 West Baltimore Street, Baltimore, Maryland 21201-1559, United States

Funder

National Cancer Institute

Tokai Pharmaceuticals, Inc.

School of Medicine, University of Maryland

Center for Biomolecular Therapeutics

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Physical and Theoretical Chemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.oprd.6b00217

Reference34 articles.

1. 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

2. Androgen Receptor Modulation Optimized for Response (ARMOR) Phase I and II Studies: Galeterone for the Treatment of Castration-Resistant Prostate Cancer

3. Discovery and Development of Galeterone (TOK-001 or VN/124-1) for the Treatment of All Stages of Prostate Cancer

4. eIF4E phosphorylation promotes tumorigenesis and is associated with prostate cancer progression

5. eIF4E Activation Is Commonly Elevated in Advanced Human Prostate Cancers and Significantly Related to Reduced Patient Survival

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3. Salinization Dramatically Enhance the Anti-Prostate Cancer Efficacies of AR/AR-V7 and Mnk1/2 Molecular Glue Degraders, Galeterone and VNPP433-3β Which Outperform Docetaxel and Enzalutamide in CRPC CWR22Rv1 Xenograft Mouse Model;Bioorganic Chemistry;2023-10

4. Discovery of a Novel Bifunctional Steroid Analog, YXG-158, as an Androgen Receptor Degrader and CYP17A1 Inhibitor for the Treatment of Enzalutamide-Resistant Prostate Cancer;Journal of Medicinal Chemistry;2023-07-17

5. Murine toxicology and pharmacokinetics of lead next generation galeterone analog, VNPP433-3β;Steroids;2023-04

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