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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Research Article

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 and Jaya Shree Anireddy*

Volume 15, Issue 2, 2018

Page: [181 - 192] Pages: 12

DOI: 10.2174/1570180814666170605115335

Price: $65

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.

Graphical Abstract


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