Synthesis and biological evaluation of sulphonyl derivatives of naturally occurring chromone alkaloid of rohitukine as anticancer agents

  • Sunil K Mishra Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow-226031, India
  • Pallavi Srivastava Department of Bioengineering, Faculty of Engineering, Integral University, Lucknow-226026, India
  • S K Rath Department of Bioengineering, Faculty of Engineering, Integral University, Lucknow-226026, India
  • A A Mahdi Department of Biochemistry, King George’s Medical University, Lucknow-226003, India
  • S K Agarwal Department of Biochemistry, King George’s Medical University, Lucknow-226003, India
  • Vijai Lakshmi KGMU, Lucknow, India
Keywords: Rohitukine, semisynthesis, Anticancer activity, Dysoxylum binectariferum, MCF-7, MDA-MB-231

Abstract

The present study deals with isolation of active constituent, rohitukine from the stem bark of Dysoxylum binectariferum, and synthesis of a series of its new sulphonyl derivatives aiming to enhance its therapeutic efficacy. Rohitukine has been isolated with more than 95% purity and ten new semisynthetic analogs have been prepared using different sulphonyl chlorides. These derivatives were evaluated for anticancer activity against MCF-7 (ER +ve) and MDA-MB-231 (ER -ve) breast cancer cell lines. Compounds K6, K8 and K10 showed significant activity against breast cancer cell lines at a concentration of 17.5 µM, 17 µM and 19 µM in MCF-7 and 20 µM, 9.8 µM and 28.5 µM in MDA-MB-231 respectively. These compounds induced significant apoptosis in MCF-cell line. Further work may enhance the anticancer activity.
Published
2018-01-20
How to Cite
Mishra, S., Srivastava, P., Rath, S., Mahdi, A., Agarwal, S., & Lakshmi, V. (2018). Synthesis and biological evaluation of sulphonyl derivatives of naturally occurring chromone alkaloid of rohitukine as anticancer agents. Journal of Basic Pharmacology and Toxicology, 2(1), 1-7. Retrieved from http://scigreen.com/index.php/JBPT/article/view/42
Section
Original Research Articles