Post Doctoral Research Fellow. Dept.of Medicinal Chemistry Univ. of Mississippi,MS,USA 20th Jan.2002-15th Jan.2003

Synthetic Organic and Medicinal Chemistry
Expertise in multistep synthesis and structure activity relationship studies of small bioactive organic molecules with potential for drug development.
Synthesis of new scaffolds / heterocyclic and hybrid molecules.

1.Design, synthesis and development of non steroidal molecules as ER modulators  (ERα / ERβ  Selective drug target leads).
Estrogen receptor modulators or antiestrogens are compounds that inhibit the action of endogenous hormones and may be potential drug targets for use in the management of post- menopausal disorders The major endogenous ligands that act at the estrogen receptors (ER) α and β are 17-β estradiol and estrone. These two estrogen receptors are members of the nuclear hormone receptor superfamily, which mediate a number of physiological processes and help in maintenance of bone health, cardiovascular system, in lowering of lipid levels and development of female reproductive systems. Post-menopausal women have severely decreased levels of endogenous estrogens and as such are often treated with HRT (hormone replacement therapy). HRT though helps in the prevention and treatment of post-menopausal syndromes such as hot flushes, mood swings etc, but it is associated, with an increased incidence of both breast and uterine cancers. Due to the drawbacks of HRT, the estrogen receptor(s) have been a target of considerable interest in the pharmaceutical industry. Synthetic non-steroidal compounds initially targeted ER α (ER β was unknown), led to development of first antibreast cancer drug ,clinically approved SERM Tamoxifen for treatment of ER+ve breast cancers. However, with subsequent studies it was found to be associated with an increased incidence of uterine cancer. Second generation ER modulators have managed to overcome this increased risk, and a new anti-osteoporotic drug raloxifene was discovered. Bazedoxifene acetate (BZA) is a new third-generation selective estrogen receptor modulator that is approved in Europe and is under  regulatory review in the United States for the prevention and treatment of postmenopausal osteoporosis.

Our group is also actively involved in the design and synthesis of new nonsteroidal heterocyclic molecules as estrogen receptor agonists/ antagonists for use in the prevention and treatment of breast cancer, osteoporosis, antifertility etc. 
2..DNA Ligase inhibitors as potential therapeutics for anticancer therapy.
DNA ligases are enzymes indispensible in various DNA repair and replication processes and inhibition of their activity can lead to an accumulation of DNA  damage and strand breaks.DNA strand break or damage at unsustainable level lead to cell death or apoptosis.
3. Design and synthesis of anticoagulants / antithrombotic agents (under THUNDER  project).

The frequency of lifestyle related diseases has increased manifolds in modern times and lifestyle disorders are emerging as silent killers. As life expectancies improve and the major causes of death and disability shift to the chronic and non communicable diseases (NCDs), populations in developing countries such as India are exposed to a new class of health risks, lifestyle disorders, arising from physical inactivity, overweight and obesity,other diet-related factors, tobacco and alcohol-related risks. The incidences of hypertension, obesity, cancer, diabetes and heart diseases are increasing at an alarming rate, especially in the young, urban population and has posed a fresh challenge to the scientific community for the development of new drugs/ molecular entities and evaluation of their biological efficacy for prevention and cure.
Currently, our group is involved in the synthesis of new coumarin based chemical entities and their testing for cardiometabolic diseases like anticoagulant activity/ antithromboembolic diseases and antidiabetic activity. The design and synthesis of new molecules and their biological evaluation will help in the generation of scientific knowledge as peer reviewed publications, patents and process or product development.

A highly efficient ultrasound-promoted synthesis of 2,3-disubstituted benzo[b]furans via intramolecular C-C bond formation in ionic liquid[bmim]BF4 at room temperature. Nisha Yadav, Mohd Kamil Hussain, Mohd.Imran Ansari, Puneet K.Gupta, K.Hajela, RSC Advances,2013,3,540-544.

Anti-tumorigenic action of 2-[piperidinoethoxyphenyl]-3-[4-hydroxyphenyl]-2H-.benzo(b)pyran: Evidence for involvement of GPR30/EGFR signaling pathway Chandra V, Fatima I, Saxena R, Hussain MK, Hajela K, Sankhwar P, Roy BG, Chandna S, Dwivedi A; Gynecology Oncology. 2013 May;129(2):433-42. IM=3.88

Silica supported perchloric acid catalysed rapid N-formylation under solvent free conditions. Mohd. Imran Ansari, Mohd Kamil Hussain, Nisha Yadav, Puneet K. Gupta and K. Hajela;.Tetrahedron Letters, 53(16), 2063-2065, 2012, (IF=2.618).

2, 3-Diaryl-2H-1-benzopyran derivatives interfere with classical and non-classical  ER signaling pathways, inhibit Akt activation and induce apoptosis in human endometrial cancer cells.  I. Fatima, V. Chandra, R. Saxena, M. Manohar, Y. Sanghani, K. Hajela, M.P.S.  Negi, P.L. Sankhwar, S.K. Jain, and A. Dwivedi ; Mol & Cellular Endocrinoloy, 348: 198-210 (2012); IM= 4.19

Anti-implantation effect of 2-[piperidinoethoxyphenyl]-3-[4-hydroxyphenyl]-2H- benzo(b)pyran, a potent antiestrogenic agent  in rats. Geetika Kharkwal,  Iram Fatima,  Shakti Kitchlu, Bishambhar Singh, K. Hajela­  & Anila Dwivedi: Fertility and Sterility), 95,(4),1322-1327, 2011,(IF=3.9).

A Simple, Fast and Efficient One Pot Synthesis of 4-Aroyl-2-pyrones: Michael Addition of Active Methylene Groups to 1,2-Diaroylacetylenes. Ravi Shankar, Uma Sharan Singh, Harsha Shukla, Vinay Thakur & K.Hajela;  Synthetic Communications, 41, (18), 2738-2746, 2011.(IF=1.0)

Eco-Friendly HClO4–SiO2 Catalyzed Synthesis of Mono- and Bis-diaryl-2H-1,4 Benzothiazines. Mohd. Imran Ansari, Ravi Shankar, Mohd. Kamil Hussain, Ruchir Kant, Prakash R. Maulik, K. Ravi Kumar &  K. Hajela. Journal of Heterocyclic Chemistry,2011,48,1336,(IF=1.0)

Apoptosis induction and inhibition of hyperplasia formation by 2-[piperidinoethoxyphenyl]-3-[4-hydroxyphenyl]-2H-benzo(b)pyran in rat uterus.Vishal Chandra; Iram Fatima;   Ruchi Saxena, Shakti Kitchlu , Sharad Sharma; Mohammad Kamil Hussain ; K. Hajela;  Preeti Bajpai  & Anila Dwivedi. American Journal of Obstetrics & Gynecology,  205(4),362.e1-e11, 2011,(IF=3.31).