P. Purushottamachar

发表

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

P. Purushottamachar, A. Khandelwal, P. Chopra, 2007, Bioorganic & medicinal chemistry.

Competitive Antagonism between the Nicotinic Allosteric Potentiating Ligand Galantamine and Kynurenic Acid at α7* Nicotinic Receptors

R. Schwarcz, E. Albuquerque, P. Purushottamachar, 2007, Journal of Pharmacology and Experimental Therapeutics.

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

P. Purushottamachar, V. Njar, Vidya P Ramamurthy, 2015, Oncotarget.

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

P. Purushottamachar, A. Khandelwal, P. Chopra, 2006, Bioorganic & medicinal chemistry.

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.

P. Purushottamachar, A. Khandelwal, L. Gediya, 2008, Journal of medicinal chemistry.

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

P. Purushottamachar, L. Gediya, O. Clement, 2012, European journal of medicinal chemistry.

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.

P. Purushottamachar, L. Gediya, T. Vasaitis, 2013, Journal of medicinal chemistry.

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

P. Purushottamachar, L. Gediya, V. Njar, 2017, Oncotarget.

Transcriptome profiling reveals that VNPP433‐3β, the lead next‐generation galeterone analog inhibits prostate cancer stem cells by downregulating epithelial–mesenchymal transition and stem cell markers

P. Purushottamachar, V. Njar, Weiliang Huang, 2022, Molecular carcinogenesis.

Novel deuterated Mnk1/2 protein degrader VNLG-152R analogs: Synthesis, In vitro Anti-TNBC activities and pharmacokinetics in mice.

P. Purushottamachar, V. Njar, E. Thomas, 2022, European journal of medicinal chemistry.

The Novel Mnk1/2 Degrader VNLG-152 Potently Inhibits TNBC Tumor Growth and Metastasis

P. Purushottamachar, L. Gediya, T. Vasaitis, 2018, bioRxiv.

Novel AR/AR-V7 and Mnk1/2 Degrader, VNPP433-3β: Molecular Mechanisms of Action and Efficacy in AR-Overexpressing Castration Resistant Prostate Cancer In Vitro and In Vivo Models

P. Purushottamachar, V. Njar, Weiliang Huang, 2022, Cells.

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

P. Purushottamachar, A. Khandelwal, L. Gediya, 2008, Bioorganic & medicinal chemistry.

Retinoids in clinical use.

P. Purushottamachar, P. Chopra, L. Gediya, 2006, Medicinal chemistry (Shariqah (United Arab Emirates)).

Autophagy Inhibition Synergistically Enhances Anticancer Efficacy of RAMBA, VN/12-1 in SKBR-3 Cells, and Tumor Xenografts

P. Purushottamachar, V. Njar, C. Daskalakis, 2012, Molecular Cancer Therapeutics.

Preclinical Development Autophagy Inhibition Synergistically Enhances Anticancer Ef fi cacy of RAMBA , VN / 12-1 in SKBR-3 Cells , and Tumor Xenografts

P. Purushottamachar, V. Njar, C. Daskalakis, 2012 .

Development of Benzimidazole Compounds for Cancer Therapy

P. Purushottamachar, V. Njar, S. Ramalingam, 2019, Chemistry and Applications of Benzimidazole and its Derivatives.

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

P. Purushottamachar, L. Gediya, T. Vasaitis, 2011, Steroids.

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

P. Purushottamachar, V. Njar, 2012, Steroids.

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

P. Purushottamachar, V. Njar, Francis N. Murigi, 2016 .

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

P. Purushottamachar, V. Njar, Vidya P Ramamurthy, 2016, ACS medicinal chemistry letters.

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

Lei Gu, Adam Ertel, Hallgeir Rui, 2015, Molecular Cancer Therapeutics.

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

P. Purushottamachar, L. Gediya, V. Njar, 2014, Oncotarget.

Murine toxicology and pharmacokinetics of lead next generation galeterone analog, VNPP433-3β

P. Purushottamachar, V. Njar, J. Beumer, 2023, Steroids.

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

P. Purushottamachar, T. Vasaitis, V. Njar, 2019, Cancers.

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.

P. Purushottamachar, V. Njar, Vidya P Ramamurthy, 2017, Oncotarget.

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.

P. Purushottamachar, P. Chopra, N. Maheshwari, 2005, Journal of medicinal chemistry.

Targeted Degradation of Androgen Receptor by VNPP433-3β in Castration-Resistant Prostate Cancer Cells Implicates Interaction with E3 Ligase MDM2 Resulting in Ubiquitin-Proteasomal Degradation

P. Purushottamachar, V. Njar, David J. Weber, 2023, Cancers.

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

P. Goss, P. Purushottamachar, L. Gediya, 2012, Breast Cancer Research and Treatment.

3D-QSAR of N-myristoyltransferase inhibiting antifungal agents by CoMFA and CoMSIA methods.

P. Purushottamachar, V. Kulkarni, Vithal M Kulkarni, 2003, Bioorganic & medicinal chemistry.

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.

P. Purushottamachar, A. Khandelwal, L. Gediya, 2014, European journal of pharmacology.

The Novel Mnk1/2 Degrader and Apoptosis Inducer VNLG-152 Potently Inhibits TNBC Tumor Growth and Metastasis

P. Purushottamachar, L. Gediya, T. Vasaitis, 2019, Cancers.

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

P. Purushottamachar, R. D. Bruno, V. Njar, 2016, The FEBS journal.

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.

P. Purushottamachar, A. Khandelwal, L. Gediya, 2008, Bioorganic & medicinal chemistry.

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.

P. Purushottamachar, V. Njar, David J. Weber, 2023, Bioorganic chemistry.

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

P. Purushottamachar, V. Njar, Vidya P Ramamurthy, 2016, ACS medicinal chemistry letters.

VNLG-152R and its deuterated analogs potently inhibit/repress triple/quadruple negative breast cancer of diverse racial origins in vitro and in vivo by upregulating E3 Ligase Synoviolin 1 (SYVN1) and inducing proteasomal degradation of MNK1/2

P. Purushottamachar, V. Njar, Vidya P Ramamurthy, 2023, Frontiers in oncology.

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

B. Leiby, N. Pattabiraman, M. Nevalainen, 2015, Molecular Cancer Therapeutics.