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

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

Volume: 15 Issue: 2

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

Affiliation:

• Centre for Chemical Sciences & Technology, Institute of Science and Technology, JNTUH, Kukatpally, Hyderabad 500085, Telangana State,India

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

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.

Cite this article as:

Kasturi Sivaprasad, Surarapu Sujatha , Uppalanchi Srinivas , Anantaraju Shilpa Hasitha , Dwivedi Shubham , Yogeeswari Perumal , Ethiraj S. Krishna and Anireddy Shree Jaya *, Synthesis of New Heteroaryl Substituted Morpholine Tagged Triazines and Evaluation of their Cytotoxic Activity, Letters in Drug Design & Discovery 2018; 15 (2) . https://dx.doi.org/10.2174/1570180814666170605115335