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Maithili A. Athavale
Godavari Academy of Science & Technology, India

The aim of the present project is to Synthesise novel derivatives of diphylline glycoside of CleistanthinA(SBGB-0001-000) and to screen them for anticancer activity (by MTT ,Soft Agar Assay) and anticancer stem cell activity (by tumorsphere assay)on Breast Cancer cell lines. In all 70 novel derivatives of SBGB-0001-000 were synthesized and screened for anticancer and anticancerstemcell activity.Out of 70,two derivatives namely, SBGB-0001-014 and SBGB-0001-023 exhibited better anticancer and anticancer stem cell activity compared to standard chemotherapeutic drug Cisplatin. Since, Cancer stem cells(CSCs)are subpopulation of cells within the cancer tissues with drug resistance and metastatic properties,these two candidates were further tested for its anticancer stem cell activity on drug(Paclitaxel)resistant population on highly metastatic breast cancer cell lineMDAMB231(with high number of CSCs)compared to standard Chemotherapeutic drug Cisplatin and a target drug therapy Sunitinib.Our sphere assay results indicate that the candidate molecules have better anticancer stem cell potential,inhibiting spheres at 25nM compared to Cisplatin and Sunitinib.”fig1” Briefly,our in-vitro data supports the anticancerstemcell effect of two novel candidates on breast cancer cell lines.Further these candidates do not exhibit any toxic effect on normal cells (peripheral blood lymphocytes)compared to Cisplatin.The molecules show good hepatocyte stability and have been taken further for the precilinal studies like PK-PD,MTD and Xenograft studies.

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