Dr. Shagufta Waseem
ASSISTANT PROFESSOR – CHEMISTRY
Department of Mathematics and Natural Sciences, School of Arts and Sciences, American University of Ras Al Khaimah, Ras Al Khaimah, United Arab Emirates
Office No.: C42
Phone: Tel. Ext. 1331
Email: shagufta.waseem@aurak.ac.ae
Biography
Dr. Shagufta joined the American University of Ras Al Khaimah as an Assistant Professor of Chemistry in the School of Arts and Sciences in August 2014. Prior to joining AURAK, Dr. Shagufta worked as an Adjunct Assistant Professor of Chemistry at the University of Modern Sciences, Dubai and American University of Ras Al Khaimah, UAE.
Dr. Shagufta also worked as a Postdoctoral Researcher Associate at the Department of Chemistry and Biochemistry, Oklahoma University, USA. She developed the noble drug delivery system for breast cancer drugs using carbon nanotubes and acquired the significant experience in nanotechnology and synthetic organic chemistry. She was appointed as a Postdoctoral Research Fellow and Visiting Scientist at Leiden/Amsterdam Centre for Drug Research (LACDR), Leiden, The Netherlands. Her research interest was In silico prediction and clinical evaluation of the cardiotoxicity of drug candidates. She was focused to identify chemical substructures as ‘chemical alerts’ that interact with this hERG channel. Dr. Shagufta received a Ph.D. under the prestigious CSIR-JRF and SRF research fellowship in Chemistry from Central Drug Research Institute (CDRI)/Lucknow University, India in 2008, her PhD research work was in the field of estrogens and antiestrogens, design and synthesis of steroidal and non-steroidal tissue selective estrogen receptor modulators (SERMs) for breast cancer, 3D-QSAR CoMFA and CoMSIA studies and analysis of pharmaceutical important molecules.
Dr. Shagufta has published 20 articles in peer-reviewed International journals of Royal Society of Chemistry, Elsevier, Wiley and Springer. Dr. Shagufta teaches courses such as General chemistry, Organic Chemistry, Chemistry in Everyday Life, and Spectroscopy along with laboratory courses.
Research and Publication
Research Interest-Dr. Shagufta
Organic Chemistry, Medicinal Chemistry focused on Breast Cancer and Osteoporosis, Heterogeneous catalysis and Nanotechnology.
Publications- Dr. Shagufta
- Irshad Ahmad and Shagufta. 2015. Recent developments in steroidal and nonsteroidal aromatase inhibitors for the chemoprevention of estrogen-dependent breast cancer. European Journal of Medicinal Chemistry, 102, 375-386.
- Irshad Ahmad and Shagufta. 2015. Sulfones: An important class of organic compounds with diverse biological activities. International Journal of Pharmacy and Pharmaceutical Sciences, 7 (3), 19-27.
- Priyanka Singh, Subal Kumar Dinda, Shagufta, Gautam Panda. 2013. Synthetic approach towards trisubstituted methanes and a chiral tertiary α-hydroxyaldehyde, possible intermediate for tetrasubstituted methanes. RSC Adv.(Royal Society of Chemistry) 3, 12100-12103. [ISSN: 2046-2069]
- Donna J. Nelson, Shagufta, Ravi Kumar. 2012. Characterization of a tamoxifen-tethered single-walled carbon nanotube conjugate by using NMR spectroscopy. Anal. Bioanal. Chem.[Springer] 404:771–776. [ISSN: 1618-2642]
- Donna J. Nelson, Ravi Kumar, Shagufta. 2012. Regiochemical reversals in nitrosobenzene reactions with carbonyl compounds – α-aminooxy ketone versus α-hydroxyamino ketone products. Eur. J. Org. Chem.(Wiley-VCH) 6013-6020. [ISSN: 1099-0690]
- Munikumar R. Reddy, Elisabeth Klaasse, Shagufta, Adriaan P. IJzerman, Andreas Bender. 2010. Validation of an in silico hERG model and its applications to the virtual screening of commercial compound databases. Chem. Med. Chem. (Wiley-VCH)5: 716-729. [ISSN: 1860-7187]
- Shagufta, Dong Guo, Elisabeth Klaasse, Henk de Vries, Johannes Brussee, Lukas Nalos, Martin B Rook, Marc A Vos, Marcel AG van der Heyden and Adriaan P. IJzerman. 2009. Exploring the chemical substructures essential for hERG K+ channel blockade by synthesis and biological evaluation of dofetilide analogues. Chem. Med. Chem.(Wiley-VCH) 4:1722-1732. [ISSN: 1860-7187]
- Shagufta, Ritesh Singh and Gautam Panda. 2009, Synthetic studies towards steroid-amino acid hybrids. Indian Journal of Chemistry.(Indian Science) 48B: 989-995. [ISSN: 0975-0983]
- Maloy K. Parai, Shagufta, Ajay K. Srivastava, Matthias Kassack, Gautam Panda. 2008. An unexpected reaction of phosphorous tribromide on chromanone, thiochromanone, 3,4-dihydro-2H-benzo[b]thiepin-5-one, 3,4-dihydro-2H-benzo[b]oxepin-5-one and tetralone derived allylic alcohols: a case study. Tetrahedron (Elsevier)64: 9962-9976. [ISSN: 0040-4020]
- Gautam Panda, Maloy Kumar Parai, Sajal Kumar Das, Shagufta, Manish Sinha, Vinita Chaturvedi, Anil K. Srivastava, Anil N. Gaikwad, Sudhir Sinha. 2007. Effect of substituents on diarymethanes for antitubercular activity. European Journal of Medicinal Chemistry (Elsevier) 42: 410-419. [ISSN: 0223-5234]
- Shagufta and Gautam Panda. 2007. A new example of a steroid-amino acid hybrid: Construction of constrained nine membered D-ring steroids. Organic and Biomolecular Chemistry (Royal Society of Chemistry) 5 : 360- 366. [ISSN 1477-0539]
- Shagufta, Ashutosh Kumar, Gautam Panda and Mohammad Imran Siddiqi. 2007. CoMFA and CoMSIA 3D-QSAR analysis of diaryloxy methano phenanthrene derivatives as anti- tubercular agents. Journal of Molecular Modeling (Springer) 13: 99-107. [ISSN:0948-5023]
- Shagufta, Ajay Kumar Srivastava, Ramesh Sharma, Rajeev Mishra, Anil K. Balapure, Puvvada S. R. Murthy and Gautam Panda. 2006. Substituted phenanthrenes with basic amino side chains: A new series of anti-breast cancer agents. Bioorganic and Medicinal Chemistry (Elsevier) 14: 1497-1505. [ISSN: 0968-0896]
- Shagufta, Ajay Kumar Srivastava and Gautam Panda. 2006. Isomerization of allylic alcohols into saturated carbonyls using phosphorus tribromide. Tetrahedron Letters (Elsevier) 47: 1065-1070. [ISSN: 0040-4039]
- Gautam Panda, Jitendra K. Mishra, Shagufta, T. C. Dinadayalane and G. Narahari Sastry & Devendra S Negi. 2006. Hard-soft acid-base (HSAB) principle and difference in d-orbital configurations of metals explain the regioselectivity of nucleophilic attack to a carbinol in Friedel-Crafts reaction catalyzed by Lewis and protonic acids. Indian Journal of Chemistry (Indian Science)45B: 276-287. [ISSN: 0975-0983]
- Shagufta, Maloy Kumar Parai and Gautam Panda. 2005. A new strategy for the synthesis of aryl- and heteroaryl-substituted exocyclic olefins from allyl alcohols using PBr3. Terahedron Letters (Elsevier) 46: 8849-8852. [ISSN: 0040-4039]
- Shagufta, Resmi Raghunandan, Prakash R. Maulik and Gautam Panda. 2005. Convenient phosphorus tribromide induced syntheses of substituted 1-arylmethylnaphthalenes from 1-tetralone derivatives. Tetrahedron Letters (Elsevier) 46: 5337-5341. [ISSN: 0040-4039]
- Gautam Panda, Shagufta, Anil K. Srivastava and Sudhir Sinha. 2005. Synthesis and antitubercular activity of 2-hydroxy-aminoalkyl derivatives of diaryloxy methano phenanthrenes. Bioorganic and Medicinal Chemistry Letters (Elsevier) 15: 5222-5225. [ISSN: 0960-894X]
- Sajal Kumar Das, Shagufta, and Gautam Panda. 2005. An easy access to unsymmetric trisubstituted methane derivatives (TRSMs). Tetrahedron Letters (Elsevier) 46: 3097-3102. [ISSN: 0040-4039]
- Shagufta, Jitendra Kumar Mishra, Vinita Chaturvedi, Anil K. Srivastava, Ranjana Srivastava and Brahm S. Srivastava. 2004. Diaryloxy methano phenanthrenes: a new class of antituberculosis agents. Bioorganic and Medicinal Chemistry (Elsevier) 12: 5269-5276. [ISSN: 0968-0896
The Food and Drug Administration (FDA) has approved several quinazoline derivatives for clinical use as anticancer drugs. These include gefitinib, erlotinib, lapatinib, afatinib, and vandetanib (Fig.1) [43]. Gefitinib (Iressa®) was approved by the FDA in 2003 for the treatment of locally advanced or metastatic non-small-cell lung cancer (NSCLC) in patients after failure of both platinum-based and/or docetaxel chemotherapies. In 2004, erlotinib (Tarceva®) was approved by the FDA for treating NSCLC. Furthermore, in 2005, the FDA approved erlotinib in combination with gemcitabine for treatment of locally advanced, unrespectable, or metastatic pancreatic cancer. Erlotinib acts as a reversible tyrosine kinase inhibitor. Lapatinib (Tykreb®) was approved by the FDA in 2012 for breast cancer treatment. It inhibits the activity of both human epidermal growth factor receptor-2 (HER2/neu) and epidermal growth factor receptor (EGFR) pathways. Vandetanib (Caprelsa®) was approved by the FDA in 2011 for the treatment of metastatic medullary thyroid cancer. It acts as a kinase inhibitor of a number of cell receptors, mainly the vascular endothelial growth factor receptor (VEGFR), EGFR, and rearranged during transfection (RET)-tyrosine kinase (TK). Afatinib (Gilotrif®) was approved by the FDA in 2013 for NSCLC treatment. It acts as an irreversible covalent inhibitor of the receptor tyrosine kinases (RTK) for EGFR and erbB-2 (HER2).
An insight into the therapeutic potential of quinazoline derivatives as anticancer agents
*Corresponding authors
Abstract
Cancer is one of the major causes of worldwide human mortality. A wide range of cytotoxic drugs are available on the market, and several compounds are in different phases of clinical trials. Many studies suggest that these cytotoxic molecules are also associated with different types of adverse side effects; therefore researchers around the globe are involved in the development of more efficient and safer anticancer drugs. In recent years, quinazoline and its derivatives have been considered as a novel class of cancer chemotherapeutic agents that show promising activity against different tumors. The aim of this article is to comprehensively review and highlight the recent developments concerning the anticancer activity of quinazoline derivatives as well as offer perspectives on the development of novel quinazoline derivatives as anticancer agents in the near future.
An insight into the therapeutic potential of quinazoline derivatives as anticancer agents
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C7MD00097A, Review Article
DOI: 10.1039/C7MD00097A, Review Article
Shagufta, Irshad Ahmad
This article reviews the recent advances in the development of quinazoline derivatives as anticancer agents.
This article reviews the recent advances in the development of quinazoline derivatives as anticancer agents.
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