Synthesis of New Heteroaryl Substituted Morpholine Tagged Triazines and Evaluation of their Cytotoxic Activity

Author(s): Sivaprasad Kasturi , Sujatha Surarapu , Srinivas Uppalanchi , Hasitha Shilpa Anantaraju , Shubham Dwivedi , Perumal Yogeeswari , Krishna S. Ethiraj , Jaya Shree Anireddy* .

Journal Name: Letters in Drug Design & Discovery

Volume 15 , Issue 2 , 2018

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Abstract:

Background: In the present study, new triazine derivatives 3, 4, 5, 6, 8 and 10 were synthesized starting from readily available cyanuric chloride 1 via nucleophilic displacement with morpholine followed by Suzuki or Stille coupling reactions and then the thermal displacement of chlorine atom with diverse substituted amines.

Methods: All synthesized compounds were screened for their cytotoxic activity against HT-29, MDA-MB-231, and HEK293 cell lines.

Results and Conclusion: Compounds 6a (IC50 (µM): 0.32 for HT-29 and 2.92 for MDA-MB-231) and 8c (IC50 (µM): 1.40 for HT-29 and 1.60 for MDA-MB-231) have been identified and compared with Doxorubicin and ZSTK474 as the reference standards.

Keywords: Cyanuric chloride, cytotoxic activity, stille coupling, suzuki reaction and triazines, doxorubicin.

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Article Details

VOLUME: 15
ISSUE: 2
Year: 2018
Page: [181 - 192]
Pages: 12
DOI: 10.2174/1570180814666170605115335
Price: $58

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