Synthesis and Invitro Anti-Cancer Evaluation of Disubstituied 1,2,4 Thiadmzole Derivatives

Shalini, S (2016) Synthesis and Invitro Anti-Cancer Evaluation of Disubstituied 1,2,4 Thiadmzole Derivatives. Masters thesis, J. K. K. Nattraja College of Pharmacy, Komarapalayam.


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INTRODUCTION: Chemistry is a very broad subject, and can justly claim to encompass many aspects of the study of biological molecules. To most researchers in the cancer fields, the term ‘chemistry’ is often used in a much narrower way and is synonymous with the synthetic chemistry as a tool for the discovery of anticancer drugs. PHARMACEUTICAL CHEMISTRY: Pharmaceutical Chemistry is an area of chemistry that deals with the structure, properties and reaction of compounds that contains carbon. Chemists in general and organic chemists in particular can create new molecules never before proposed which, if carefully designed, may have important properties for the betterment of the human experience. One of the main objectives of organic and medicinal chemistry is the design, synthesis and production of molecule having value as human therapeutic agents1. The department of pharmaceutical chemistry is to impart in depth knowledge about all the chemical aspects of drugs and natural products, such as the structure, synthesis, isolation and structural activity relationship with the pharmacological activity. AIMS & OBJECTIVES OF THE PRESENT STUDY: 1.To synthesize a series of novel 2, 5-disubstituted thiadiazoles. 2. To characterize the synthesized compounds by IR, NMR, Mass spectra and elemental analysis.3.To evaluate the test compounds for in vitro anti-cancer activity by MTT IN VITRO ASSAY METHOD.SUMMARY AND CONCLUSION:In summary, a new series of substituted N-(5-aryl-1, 3, 4-thiadiazole-2-yl)-2- alkyl / aryl substituted acetamides were synthesized. These title compounds containing ten different substituents at C-2 and C-5 were screened for their anticancer agents. Most of the test compounds were found to exhibit significant anticancer activity against the human cervical cancer cell line (HeLa) in the highest concentration. Among the substituents at C-2, dimethyamino substituent and at C-5 4-methyl phenyl substitutent showed maximum potency, while morpholino and pyrolidine substitutent showed equipotent activity but the piperidine substituent at C-2 exhibited least activity when compare to other substituents. The order of activity at C-2 is dimethyamino ≥ morpholine ≥ imidazole ≥ pyrolidine ≥ piperidine group and at C-5 is 4-methyl ≥ 4- bromo group. Among the test compounds, compound 2-(dimethylamino)-N-(5-p-tolyl-1,3, 4-thiadiazol-2-yl)acetamide (TZ1) was found to be the most active agent which showed 74.85 percentage of cell inhibition against the human cervical cancer cell line (HeLa) in the highest concentration, which have dimethylamino group in the thiadiazole nucleus. Hence this molecule can be selected as a lead molecule of the present study for further exploitation.

Item Type: Thesis (Masters)
Additional Information: REG NO. 261315208
Uncontrolled Keywords: Synthesis ; Invitro Anti-Cancer ; Disubstituied 1,2,4 ; Thiadmzole Derivatives
Subjects: PHARMACY > Pharmaceutical Chemistry
Depositing User: Ravindran C
Date Deposited: 19 Mar 2018 08:43
Last Modified: 21 Mar 2018 08:04

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