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Title: Synthesis of Some new Hybrid Heterocyclic Molecules and Evaluation of their In Vitro Cytotoxic Activities
Researcher: Arunkumar Thiriveedhi
Guide(s): R. Venkata Nadh , N. Srinivasu
University: Vignans Foundation for Science Technology and Research
Completed Date: 2018
Abstract: According to World Health Organisation (WHO), the deaths caused due to the cancer are very high than the malaria, tuberculosis and AIDS across the world in 2010. Hybrid drug molecules exhibit a noteworthy role in pharmacology because of low toxicity and selectivity. Hence, in the present study, it is proposed to synthesize and study antitumor applications of four different hybrid derivatives. newlineSynthesized a novel sequence of isoxazole-chalcone hybrids (85a-m) and studied their cytotoxic activities. 85a, 85b, 85e, 85i, 85j and 85k exhibited potency towards cell lines of prostate (DU-145) and the observed cytotoxic studies were related to the presence of electron donating groups like methoxy on either of phenyl rings. Out of the synthesized eighteen quinazoline linked chalcones, three (98f, 98g and 98h) have shown notable cytotoxicity against leukemia, non-small lung, colon and breast cell line respectively. Among the synthesized a new sequence of pyrazole core structure conjugates with benzoxazole moieties (114a-j), 114c and 114b demonstrated admirable anticancer potency (GI50 lt0.1 and#956;M) towards A549 and MCF-7. The molecular docking studies proved them to be able to interfere with the role of ATP-Src tyrosine kinase protein. Pyrimidine-pyrrole appended substituted triazole derivatives (126a-l) are active and display reasonable to good activity towards selected cell lines. Higher activity was observed with polar substituents (pyradizine, hexanol dichlorobenzene, chloro propane, methoxy methyl benzene) on triazole dictates. The observed activity profile suggested that electron withdrawing groups on triazole heterocycle improved the anticancer activity. newline newline
Pagination: 218
Appears in Departments:Division of Chemistry

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