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

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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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