Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry


Synthesis and Biological Evaluation of Sulphonyl Derivatives of Naturally Occurring Chromone Alkaloid of Rohitukine as Anticancer Agents

Author(s): Sunil K Mishra, Pallavi Srivastava, Rath SK, Mahdi AA, Agarwal SK, Lakshmi V

Aim: The present study deals with isolation of active constituent rohitukine from stem bark of Dysoxylum binectariferum, and synthesis of a series of its new sulphonyl derivatives aiming to enhance its therapeutic efficacy.

Experimental: Rohitukine has been isolated to >95% purity and ten new semisynthetic analogs have been prepared using different sulphonyl chlorides. These derivatives were evaluated for anticancer activity against Breast Cancer Cell Line (MCF-7) (ER +ve) and MDA-MB-231 (ER -ve) breast cancer cell lines.

Major findings: 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, 19.8 μM and 28.5 μM in MDA-MB-231 respectively.

Conclusion: These compounds induced significant apoptosis in MCF-cell line. Further work may enhance the anticancer activity.

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