Discovery of 4-methyl-2-oxo-2H-chromen-7-yl-2-benzamidoacetate as Anti-proliferative Agents
Journal Title: International Journal of Ayurveda and Pharmaceutical Chemistry - Year 2018, Vol 0, Issue 0
Abstract
Coumarin scaffolds are well known for exhibiting tremendous anti-tumor activity. The present work involved synthesis of a coumarin hybrid utilizing hippuric acid and screening of its antineoplastic potential. The coumarin scaffold (3) was fabricated utilizing the PechmanCondensation method. In this method, the phenolic derivative (1) and 3-keto esters (2) were made to react in the presence of a Lewis acid catalyst (Conc. H2SO4). To facilitate substitution at the 7th position of the coumarin scaffold, the hydroxyl group was replaced by the chloride function utilizing POCl3. In the ultimate step, hippuric acid (5) was made to react in the presence of conc. HCl to form hippuric acid-coumarin hybrid (6). The in vitro anti-cancer screening was performed against breast cancer cell line MCF-7 employing Sulforhodamine B (SRB) assay. The study represented the synthesis of coumarin hybrid utilizing hippuric acid. The spectroscopic, physicochemical, and elemental analyses data were found to be quite complimentary to the proposed structures. The compound showed a very promising anti-cancer activity (IC50 value of 31.88 μM) as compared to the marketed drug capecitabine (IC50 value of 6.87 μM). The study will surely endorse investigators across the globe in designing more analogs with pronounced activities in coming future
Authors and Affiliations
Chitralekha Deorao Padole, Mrunali Digambar Amdare, Kamna Rajesh Jogdand, Latika Liladhar Kathane, Nutan Ganesh Kuhite, Debarshi Kar Mahapatra
Keywords
Related Articles
- EP ID EP295216
- DOI -
- Views 86
- Downloads 0
Role of Brihatyadi Taila Gandusha in the Management of Krimi Danta (Dental Caries)
The importance has been given to Dental hygiene to maintain health and beauty. The healthy teeth are very much necessary for healthy body. The disease, Krimi Danta is considered under Danta roga. Krimi Danta is character...
A Comparative Clinical Study to Evaluate the Efficacy of Jalaukāvacārana and Siddārthakādi Lepa in the Management of Mukhadūṣikā w.s.r. to Acne Vulgaris
Mukhadūṣikā, having a symptomatic correlation with Acne vulgaris, is one of the most challenging and stubborn skin disorder prevailing since Vaidika era. It affects approximately 80% of the adolescents around the world....
A Conceptual Study on Effect of Virechan Karma with Trivruttadi Yog in Management of Amlapitta
Amlapitta is a disease of Annavah strotas (gastrointestinal tract). This disease is described in classical ayurvedic texts. The excess formation of vitiated pitta due to improper diet and lifestyle habits is the main cau...
A Short Review on KshudraRoga
The skin is the largest protective organ of the body between the external environment and internal environment of the body. It has several layers and appendages. The diseases which manifest on the skin is called skin dis...
Clinico-comparative Study of Trayodasanga Guggulu with and without Nasya Karma in the Management of Avabahuka (Frozen Shoulder Syndrome)
INTRODUCTION Frozen shoulder (adhesive capsulitis - capsule thickens and tightens around the shoulder joint, restricting its movement) is a condition characterized by stiffness and pain in the shoulder joint. non-steroid...