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Vincent C.O Njar
 

Vincent C.O Njar Ph.D.

Academic Title: Professor
Primary Appointment: Pharmacology
Additional Title(s): Professor of Medicinal Chemistry and Pharmacology; Head, Medicinal Chemistry Section, Center for Biomolecular Therapeutics (CBT)
vnjar@som.umaryland.edu
Location: HSF1, 580 E
Phone: (410) 706 6364 (Office)
Fax: (410) 706 0032
Cell: (443) 996 0536
Lab: (410) 706 6365

Personal History

Dr. Vincent Njar completed his B. Sc. in Chemistry at University of Ibadan (Nigeria) in 1976 and went on to obtain a Ph.D. in Organic Chemistry in 1980 from University College London (UK) under the supervision of Derek V. Banthorpe. Following two years of postdoctoral research with the late Eliahu Caspi at Worcester Foundation for Experimental Biology, Shrewsbury, Mass. (USA), he joined the Department of Chemistry at the University of Ibadan (Nigeria) as Lecturer II. He was promoted through the ranks and became Professor of Organic Chemistry in 1996.

During his tenure at University of Ibadan, he was visiting Professor at several institutions, including: Johns Hopkins University, Baltimore, USA (1988, 1989, 1992 & 1993); Universite de Sherbrooke, Sherbrooke, Quebec, Canada (1990); University of Southampton, Southampton, UK (1991, 1992 & 1995); and University of Saarland, Saarbruecken, Germany (1994-1995). During these research visits he collaborated with eminent scholars including: Professors Eliahu Caspi (Worcester Foundation), Cecil Robinson (Johns Hopkins), Liat Tan (Sherbrooke), Muhammad Akhtar (Southampton) and Rolf Hartmann (Saarland). Theses research visits were made possible by grant and fellowship awards from US National Institutes of Health, Bethesda, USA; (Fogarty International Research Fellowship) International Union Against Cancer, Geneva, Switzerland; Medical Research Council of Canada; Alexander von Humboldt Foundation, Bonn, Germany (Alexander von Humboldt Fellowship) and Wellcome Trust Foundation, London, UK.

Following several research visits from 1996 to 1998 collaborating with Dr. Angela Brodie at University of Maryland, Baltimore (UMB), he was appointed Assistant Professor of Pharmacology in 1999 and was promoted to Associate Professor in 2002. In 2008, Dr. Njar was appointed Professor of Medicinal Chemistry and Oncopharmacology at Jefferson School of Pharmacy, Thomas Jefferson University, Philadelphia, PA, USA. Finally, in January 2012, he came back to UMB as Professor of Medicinal Chemistry and Pharmacology and Head, Medicinal Chemistry Section of the newly established Center for Biomolecular Therapeutics (CBT).

Dr. Njar actively participates in several drug discovery and development grant review committees and he is a Charter Member of NIH/NCI’s Drug Discovery and Molecular Pharmacology (DMP) Grant Review Study Section; NIH/NCI’s Small Business Cancer Drug Development and Therapeutics (CDDT) Study Section and Scientific Reviewer for US Department of Defense (DOD) Prostate and Breast Cancer Research Programs. He is also grant reviewer for several foreign agencies in the United Kingdom, Australia, Singapore and Qatar. His research is currently supported by the US National Institutes of Health (NIH), the National Cancer Institute (NCI) and US Veteran Administration (VA).

Research Interests

Dr. Vincent C. O. Njar has a long standing interest in the rational discovery and development of small molecules as anti-cancer agents. The major objective of my current research is to design, synthesize, and evaluate novel patentable compounds in suitable model systems with potentials to prevent and/or treat breast and prostate cancers. I am also interested in understanding mechanisms of anti-cancer actions of the novel agents. My research is at the interface of medicinal chemistry and pharmacology/oncology. My research is interdisciplinary and has strong therapeutics translational potentials. My overall research strategy is presented in the schematic below.

Lab Techniques and Equipment

Organic & Medicinal Chemistry (small molecule synthesis, NMR, IR, HRMS, HPLC, UHPLC), Molecular Modeling, Oncopharmacology (prostate and breast cancers), Molecular Biology, In Vivo novel agents testing (toxicology, preliminary pharmacokinetics, anti-tumor efficacy assessments) techniques are used in Dr. Njar’s Laboratory.


Laboratory Personnel:

Current Personnel:

  • Dr. Lalji Gedeya, Ph.D., - Research Associate
  • Dr. Puranik Purushottamachar, Ph.D., - Research Associate
  • Dr. Senthilmurugan Ramalingam, Ph.D., - Postdoctoral Fellow
  • Dr. Hannah Mbatia, Ph.D., - Postdoctoral Fellow
  • Dr. Vidya Ramamurthy, Ph.D., - Postdoctoral Fellow
  • Mr. Andrew Kwegyir-Afful, MS, - Graduate Student
  • Mr. David McCarty, BS, - Graduate Student
  • Ms. Marlena Martin, BS, - Research Technician

Former Students and Postdoctoral Fellows/Research Associates

  • Dr. Taiwo Womoloju - (Former Student)
  • Dr. Julius Adesanwo - (Former Student)
  • Dr. Isiaka Oguwande - (Former Student)
  • Dr. Amba Ayambem - (Former Student)
  • Dr. Markus Hector (co-Advisor) - (Former Student)
  • Dr. Carlic Huynh - (Former Student)
  • Dr. Jyoti Patel - (Former Student & Postdoctoral Fellow)
  • Dr. Aashvini Belosay - (Former Postdoctoral Fellow)
  • Dr. Pankaj Chopra (Former Student)
  • Dr. Neha Maheshwari - (Former Postdoctoral Fellow)
  • Dr. Tadas Sean Vasaitis (co-Advisor) - (Former Student)
  • Dr. Vania Moreira (co-Advisor) - (Former Student)
  • Dr. Aakanksha Khandelwal - (Former Student & Postdoctoral Fellow)
  • Dr. Robert Bruno - (Former Student)
  • Dr. Abhijit Godbole - (Former Student& Postdoctoral Fellow)
  • Dr. Bianca Gomez - (Former Postdoctoral Fellow)
  • Dr. Quigyuan Yang - (Former Research Associate)
  • Ms. Jhalak Mehta - (Former Student)

Research Projects:

1. Novel Retinoic Acid Metabolism Blocking Agents (RAMBAs) for Breast and Prostate Cancers:

We have recently designed and synthesized novel inhibitors of all-trans retinoic acid (ATRA) metabolism enzyme (CYP26). These inhibitors are also referred to as retinoic acid metabolism blocking agents (RAMBAs). Some of our compounds are by far the most potent RAMBAs known. These inhibitors may be useful in enhancing the levels of endogenous ATRA, causing ‘ATRA-mimetic’ effects without the need for ATRA administration. Some of our novel RAMBAs are potent inhibitors of growth of both breast and prostate cancer cells and they are also strong inhibitors of breast cancer tumors in animal xenograft models. Our lead multi-target RAMBA, VN/14-1 may be useful for the treatment of endocrine-sensitive and –insensitive breast cancer. Our RAMBAs (VN/14-1) technology has recently been licensed to Cancer Research UK, London, United Kingdom for advanced pre-clinical studies in view of Phase I clinical trials in breast cancer patients.

In both breast and prostate cancer cell lines and tumor xenografts, we have found that combination of our RAMBAs with histone deacetylase inhibitors (HDACIs) result in additive/synergistic cell/tumor growth inhibition. The combination of VN/66-1 and MS-275 is highly effective in both hormone-dependent (LNCaP) and –independent (PC-3) prostate cancer. The technology of/around VN/66-1 will soon be licensed for further development.

Recently, we reported that our RAMBA VN/12-1 induces autophagy and apoptosis and inhibits the growth of SKBR-3 xenografts by 80-90%. We also showed that combination of VN/12-1 with autophagy inhibitor, chloroquine was beneficial. Some of the new projects in the laboratory also involve pharmacological testing our novel RAMBAs against triple-negative breast cancer cell lines and neuroblastoma cell lines. We believe that our RAMBAs have potential to find important application as therapeutic agents in oncology and dermatology. Research on the combination of retinoids and/or RAMBAs with histone deacetylase inhibitors and DNA methylation inhibitors is also being pursued. Another recent interest is to develop new non-retinoidal RAMBAs. In this regard, we developed the first chemical feature-based pharmacophore model of potent retinoidal retinoic acid metabolism blocking agents (RAMBAs), which enabled us to identify novel RAMBAs scaffolds. This new pharmacophore model can now be used for virtual screening of other robust database that should lead to the identification of highly potent RAMBAs with hitherto unknown scaffolds. It is important to note here that our success in the syntheses of new compounds continues to benefit from a novel synthetic method that I invented in 1999, which enables the synthesis of novel C4-azolyl retinoids (see Scheme below; Njar VCO et al., Bioorg. Med Chem. Lett., 2000, 10: 1905-1908).

Ongoing Studies:

On the basis of recent studies, we have determined that our lead compounds, VN/14-1 and its methyl ester, VN/12-1 are fairly toxic in mice. In addition, we have also identified an inactive/toxic polymorph of VN/14-1, following large-scale production. These undesirable activities limit their usefulness. Consequently, we are currently synthesizing novel RAMBA retinamides, which are significantly less toxic than VN/12-1 and VN/14-1. We are exploring the usefulness of these agents in the treatment of breast and prostate cancers. Current projects include rationale design, synthesis and characterization of compounds in attempts to further improve their drug-like properties. Following cell growth inhibition and colony formation assays, lead compounds are subjected to rigorous mechanistic studies to understand how these cancer cells are inhibited. Thereafter, the promising compounds will be tested in appropriate animal xenograft models of breast and prostate cancers. New compounds of this project are code named VNLG-- or VNHM-- compounds.

2. Inhibitors of Androgen Synthesis (17α-Hydroxylase/17,20-lyase; CYP17) /Anti-androgens/Androgen Receptor Down-regulating Agents.

In collaboration with Dr. Angela Brodie, we have developed some of the most potent inhibitors of CYP17 known. Some of these novel CYP17 inhibitors are also potent androgen receptor (AR) antagonists (anti-androgens) and cause strong AR degradation. Our lead VN/124-1 is more effective than castration or clinically used antiandrogen (bicalutamide) in suppressing tumor growth and also in preventing their development in LAPC-4 human prostate cancer model. We recently discovered that a clinically used HDACI, vorinostat (SAHA) acts synergistically with VN/124-1 to inhibit AR+ androgen-sensitive and –insensitive LNCaP prostate cancer cell proliferation. Quite unexpectedly, VN/124-1 strongly inhibits proliferation of AR- PC-3 prostate cancer cells. Subsequent mechanistic studies lead to the identification of induction endoplasmic reticulum (ER) stress response as its other mechanism of action. So far, VN/124-1 has at least 4 mechanisms of action, including: CYP17 inhibition, AR antagonism, AR degradation and induction of ER stress response as depicted below.

Our CYP17/antiandrogen technology was licensed to Tokai Pharmaceuticals, Inc. Cambridge, MA in 2006 with the goal of evaluating the impact of VN/124-1 in patients with prostate cancer. Indeed, VN/124-1 (TOK-001 or Galeterone) has recently successfully completed phase I/II clinical trials in castration-resistant prostate cancer patients. On June 12, 2012 Galeterone received Fast Track designation from the U.S. Food and Drug Administration (FDA) for the potential treatment of metastatic castration-resistant prostate cancer (CRPC). Large phase II clinical trials in CRPC patients started on December 17, 2012. Here again, as with the RAMBAs projects, our success in the syntheses of new compounds continues to benefit from a novel synthetic method that I invented in 1996, which enables the synthesis of novel C17-benzimidazole  (see Scheme below; Njar VCO et al., Bioorg. Med Chem. Lett., 1996, 6: 2777-2782; Njar VCO et al., J. Med. Chem., 1998, 41: 902-912).

Ongoing Studies:

In this project our current focus is to use VN/124-1 as a lead to develop a novel class of AR down-regulating agents (ARDAS) through lead optimization and molecular modeling or computer aided drug design strategies. In addition, structural studies and solving X-ray crystal structures of AR in the presence and absence of VN/124-1 and new analogs as well as structural NMR studies are in progress. In this effort, we have an abstract, a manuscript (in press, JMC) and two provisional US patent applications that reports on the discovery of VN/124-1 analogs that are ~ 4-fold more potent than VN/124-1. We are also investigation the mechanism of VN/124-1/new analogs/mimetics-induced AR degradation. The promising compounds will be tested in appropriate animal models of castration resistance prostate cancer and PC metastasis. New compounds of this project are code named VNLG-- or VNPP-- compounds.


Publications

Selected Recent Publications

Njar VCO, Safi E, Silverton JV, Robinson CH. Novel 10β-aziridinyl steroids; inhibitors of aromatase. J. Chem Soc. Perkin Trans. 1. 1993:1161-1168.

Akhtar M, Njar VCO, Wright JN. Mechanistic studies on aromatase and related C-C bond cleaving P-450 enzymes. J. Steroid Biochem. Molec. Biol., 1993, 44:375-387.

Njar VCO, Hector M, Hartmann RW. 20-Amino and 20,21-aziridinyl pregnane steroids: Development of potent inhibitors of 17α-hydroxylase/C17,20-lyase (P-45017α). Bioorg. Med. Chem., 1996, 61:1447-1453.

Njar VCO*, #, Klus GT, Brodie AMH. Nucleophilic vinylic “addition-elimination” substitution reaction of 3β-acetoxy-17-chloro-16-formylandrosta-5,16-diene: A novel and general route to 17-substituted-∆16 steroids. Part 1. Synthesis of novel 17-azolyl-∆16 steroids; inhibitors of 17α-hydroxylase/17,20-lyase (17α-lyase). Bioorg. Med. Chem. Lett., 1996, 6:2777-2782.

Njar VCO, Kato K, Nnane IP, Grigoryev DN, Long BJ, Brodie, A. M. H. Novel 17-azolyl steroids; potent inhibitors of cytochrome 17α-hydroxylase/17,20-lyase (P45017α): Potential agents for the treatment of prostate cancer. J. Med. Chem., 1998, 41:902-912.

Njar VCO*, #, Nnane IP, Brodie AMH. Potent inhibition of retinoic acid metabolism enzyme(s) by novel azolyl retinoids. Bioorg. Med. Chem. Lett., 2000, 10:1905-1908.

Njar V. C. O*, #. High-yield synthesis of novel imidazoles and triazoles from alcohols and phenols. Synthesis, 2000, 14:2019-2028.

Patel J, Huynh C, Handratta VD, Gediya LK, Brodie AMH, Goloubeva OG, Clement OO, Nnane IP, Soprano DR, Njar VCO. Novel Retinoic Acid Metabolism Blocking Agents (RAMBAs) 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. J. Med. Chem., 2004, 47:6716-6729.

Handratta VD, Vasaitis TS, Njar VCO#, Kataria R, Chopra P, Newman Jr. D, Farquhar, R, Brodie AMH.# Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens: Synthesis, Pharmacokinetics and Antitumor Activity in the LAPC4 Human Prostate Cancer Xenograft Model. J. Med. Chem., 2005, 48:2972-2984.

Gediya LK, Chopra P, Purushottamachar P, Njar VCO. A New simple and high-yield synthesis of Suberoylanilide Hydroxamic Acid (SAHA) and Its Inhibitory Effect alone or in Combination with Retinoids on Proliferation of Human LNCaP Prostate Cancer Cells. J. Med. Chem., 2005, 48:5047-5051.

Huynh CK, Brodie AMH, Njar VCO. Inhibitory effects of retinoic acid metabolism blocking agents (RAMBAs) on the growth of human prostate cancer cells and LNCaP prostate tumor xenografts in SCID mice. Br. J. Cancer, 2006, 94:513-523.

**Njar VCO*, #, Gediya L, Purushottamachar P, Chopra P, Vasaitis TS, Khandelwal A, Mehta J, Huynh C, Belosay A, Patel J. Retinoic acid metabolism blocking agents (RAMBAs) for treatment of cancer and dermatological diseases. Bioorg. Med. Chem., 2006, 14:4323-4340.
**(1. This review article that appeared on July 1, 2006, was recognized as a “top-25 most downloaded” article from Bioorganic & Medicinal Chemistry (BMC) on ScienceDirect during 2006. 2. Recently, this article has been recognized in the “top-50 most cited article” as published in Bioorganic & Medicinal Chemistry 2005-2008). 3. This paper was recognized as a Best Paper 2006-2009.

Njar VCO*, #, Gediya L, Purushottamachar P, Chopra P, Belosay A, Patel J. Retinoids in clinical use. Med. Chem., 2006, 2:431-438.
Guo Z., Dai B, Jiang T, Xu K, Xie Y, Kim O, Nesheiwat I, Kong X, Melamed J, Handratta VD, Njar VCO, Brodie AMH, Yu L-R, Veenstra TD, Chen H, Qiu Y. Regulation of the androgen receptor activity by tyrosine phosphorylation. Cancer Cell, 2006, 10:309-319.

Belosay A, Brodie AMH, Njar VCO. Effects of novel retinoic acid metabolism blocking agent (VN/14-1) letrozole insensitive breast cancer cells. Cancer Res., 2006, 66:11485-11493.

Patel JB, Khandelwal A, Handratta VD, Chopra P, Njar VCO. Murine toxicology and pharmacokinetics of novel retinoic acid metabolism blocking agents (RAMBAs). Cancer Chemother. Pharmacol., 2007, 60:899-905.

Patel JB, Mehta J, Belosay A, Sabnis G, Khandelwal A, Brodie AMH, Soprano DR, Njar VCO. Novel retinoic acid metabolism blocking agents have potent inhibitory activities on human breast cancer cell and tumor growth. Br. J. Cancer, 2007, 96:1204-1215.

Purushottamachar P, Khandelwal A, Chopra P, Maheshwari N, Gediya LK, Vasaitis TS, Bruno RD, Clement OO, Njar VCO. First pharmacophore-based identification of androgen receptor down-regulating agents: discovery of potent anti-prostate cancer agents. Bioorg. Med. Chem., 2007, 15:3413-3421.

**Bruno RD, Njar VCO. Targeting cytochrome P450 enzymes: A new approach in anti-cancer drug development. Bioorg. Med. Chem., 2007, 15:5047-5060.
** This paper was recognized as a Best Paper 2006-2009.

Lopes C, Pereira EFR, Wu H-U, Purushottamachar P, Njar VCO, Schwarcz R, Albuquerque EX. Competitive Antagonism between the Nicotinic Allosteric Potentiating Ligand Galantamine and Kynurenic Acid at α7* Nicotinic Receptors. Pharmacol. Exp. Ther., 2007, 322:48-58.

Moreira VMA, Vasaitis TS, Njar VCO#, Salvador JAR.# Synthesis and evaluation of novel 17-indazole androstene derivatives designed as CYP17 inhibitors. Steroids, 2007, 72:939-948.

Gediya LK, Belosay A, Khandelwal A, Purushottamachar P, Njar VCO. 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. Bioog. Med. Chem., 2008, 16:3352-3360.

Schayowitz A, Sabnis G, Njar VCO, Brodie AMH. Synergistic effect of a novel antiandrogen, VN/124-1 and signal transduction inhibitors in prostate cancer progression to hormone independence in vitro. Mol. Cancer Ther., 2008, 7:121-132.

Purushottamachar P, Khandelwal A, Vasaitis TS, Bruno RD, Gediya LK, Njar VCO. Potent anti-prostate cancer agents derived from a novel androgen receptor down-regulating agent. Bioog. Med. Chem., 2008, 16:3519-3529.
Khandelwal A, Gediya LK, Njar VCO. MS-275 synergistically enhances the growth inhibitory effects of RAMBA VN/66-1 in hormone-insensitive PC-3 prostate cancer cells and tumors. Br. J. Cancer 2008, 98:1234-1243.

Moreira VM, Salvador JAR#, Vasaitis TS, Njar VCO#. CYP17 inhibitors for prostate cancer treatment – An update. Curr. Med. Chem., 2008, 15:868-899.

Vasaitis TS, Belosay A, Schayowitz A, Khandelwal A, Chopra P, Gediya LK, Guo Z, Fang H-B, Njar VCO#, Brodie AMH.# Androgen receptor inactivation contributes to antitumor efficacy of CYP17 inhibitor VN/124-1 in prostate cancer. Mol. Cancer Ther., 2008, 7:2348-2357.

Gediya LK, Khandelwal A, Patel JB, Belosay A, Sabnis G, Mehta J, Purushottamachar P, Njar VCO. 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. J. Med. Chem., 2008, 51:3895-3904.
Moreira VMA, Vasaitis TS, Njar VCO#, Salvador JAR#. Synthesis of novel C17 steroidal carbamates. Studies on CYP17 action, androgen receptor binding and function, and prostate cancer cell growth. Steroids, 2008, 73:1217-1227.

Bruno RD, Gover TD, Burger AM, Brodie A, Njar VCO. 17α-Hydroxylase/17,20-lyase inhibitor VN/124-1 inhibits growth of androgen-independent prostate cancer cells via induction of the endoplasmic reticulum stress response. Mol. Cancer Ther., 2008, 7:2828-2836.

Njar VCO. Retinoids in clinical use. In: “Nuclear Receptors as Drug Targets”, E. Ottow and H. Weinmann (Eds.), WILEY-VCH Veriag & Co. KGaA, Weinheim, 2008, volume 39, chapter 12, 389-408.

Brodie A, Njar V, Macedo LF, Vasaitis TS, Sabnis G. The Coffey Lecture: Steroidogenic enzyme inhibitors and hormone dependent cancer. Urol. Oncol., 2009, 27:53-63.

Dexheimer TS, Gediya LK, Stephen AG, Weidlich I, Antony S, Marchand C, Interhal H, Nickaus M, Fisher RJ, Njar VC, Pommier Y. 4-Pregnen-21-ol-3,20-dione-21-(4-bromobenzenesufonate) (NSC 88915) and related novel steroid derivatives as tyrosyl-DNA phosphodiesterase (Tdp1) inhibitor. J. Med. Chem., 2009, 52:7122-7131.

Gediya LK, Njar VCO. Promise and challenges in drug discovery and development of hybrid anticancer drugs. Expert Opin. Drug Discov., 2009, 4:1099-1111.

Vasaitis TS, Njar VCO. A review of novel, potent antiandrogens of therapeutic potential: recent advances and promising developments. Future Medicinal Chemistry, 2010, 2:667-680.

Swanson HI, Njar VCO, Yu Z, Castro DJ, Gonzalez FJ, Williams DE, Haug Y, Kong AT, Doloff JC, Ma J, Waxman DJ, Scott EE. Targeting drug-metabolizing enzymes for effective chemoprevention. Drug Metab Dispos., 2010, 38:539-544.

Schayowitz A, Sabnis G, Goloubeva O, Njar VCO#, Brodie AMH.# Prolonging hormone sensitivity in prostate cancer xenografts through dual inhibition of AR and mTOR. Br. J. Cancer, 2010, 103:1001-1007.

Vasaitis TS, Bruno RD; Njar VCO. CYP17 inhibitors for prostate cancer therapy. J. Steroid Biochem. Mol. Biol., 2011, 125:23-31.

Bruno RD, Vasaitis TS, Gediya LK, Purushottamachar P, Godbole AM, Ates-Alagoz, Z, Brodie AMH, Njar VCO. Synthesis and biological evaluations of putative metabolically stable analogs of VN/124-1 (TOK-001) analogs: Head to head anti-tumor efficacy evaluation of VN/124-1 (TOK-001) and abiraterone in LAPC-4 human prostate cancer xenograft model. Steroids, 2011, 76:1268-1279.

Godbole AM, Njar VCO. New insights into androgen targeted therapies and epigenetic therapies in prostate cancer. Prostate Cancer, 2011, Article ID 918707,13 pages, doi:10.1155/2011/918707

Godbole AM, Njar VCO. Prostate Cancer: Current and emerging therapies, Current Cancer Treatments – Novel Beyond Conventional Approaches, Oner Ozdemir (Ed) (ISBN 978-953-307-397-2) Available from: http://www.intechopen.com/articles/show/title/prostate-cancer-current-and-emerging-therapies July 2011

Goss PE., Qi S, Hu H, Gediya LK., Purushottamachar P, Godbole AM., Njar VCO. Anti-tumor effects of a novel retinoic acid metabolism blocking agent VN/14-1 in the N-methyl-N-nitrosourea (MNU)-induced rat mammary carcinoma model and its effects on the uterus. Breast Cancer Res. Treat., 2012, 133: 137-144.

Purushottamachar P, Patel JB, Gediya LK, Clement OO, Njar VC. First chemical feature-based pharmacophore modeling of potent retinoidal retinoic acid metabolism blocking agents (RAMBAs): Identification of novel RAMBA scaffolds. Eur J Med Chem. 2012, 47: 412-423.

Godbole AM, Purushottamachar P, Martin MS, Daskalakis C, Njar VC. Autophagy inhibition synergistically enhances anticancer efficacy of RAMBA, VN/12-1 in SKBR-3 cells, and tumor xenografts. Mol Cancer Ther. 2012, 11: 898-908.

Godbole AM, Purushottamachar P, Martin MS, Njar VC. Murine toxicology and pharmacokinetics evaluation of retinoic acid metabolism blocking agent (RAMBA), VN/12-1. Cancer Chemother Pharmacol. 2012, 70: 339-344.

Tran K, Risingsong R, B Royce D, Williams CR, Sporn MB, Pioli PA, Gediya LK, Njar VC, Liby KT. The combination of the histone deacetylase inhibitor vorinostat and synthetic triterpenoids reduces tumorigenesis in mouse models of cancer. Carcinogenesis, 2013, 34:199-210. PMID: 23042302.

Purushottamachar P, Njar VC. A new simple and high-yield synthesis of 5α-dihydrotestosterone (DHT), a potent androgen receptor agonist. Steroids, 2012; 77: 1530-1534. PMID: 23044354.

Ramalingam S, Godbole AM, Njar VCO. Modulation of intracellular signaling circuits by dietary food constituents: facts and fantasies for cancer prevention and therapy. In: Food as Medicine. Essa MM, Memon MA (eds); New York. Nova Science Publishers, Inc. 2013, 375-390.

Godbole AM, Ramalingam S, Njar VCO. Role of dietary polyphenols in cancer prevention by epigenetic modulation.In: Food as Medicine. Essa MM, Memon MA (eds); New York. Nova Science Publishers, Inc. 2013, 375-390.

Purushottamachar P, Godbole AM, Gediya LK, Marlena S. Martin MS, Vasaitis TS, Kwegyir-Afful AK, Ates-Alagoz Z, Njar VCO. Systematic Structure Modifications of Multi-target Prostate Cancer Drug Candidate Galeterone to Produce Novel Androgen Receptor Down-regulating Agents as an Approach to Treatment of Advanced Prostate Cancer. J. Med. Chem., 2013, In Press.

Selected Patents & Intellectual Properties (Inventions and Licenses)

Dr. Vincent Njar holds thirteen patents from the US and several other countries and has thirty nine active Intellectual Property and Licensing Activities as of February 28, 2013 with University of Maryland, Baltimore Office of Research and Development.