Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 26, Issue 17, Pages 4916-4929Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2018.08.031
Keywords
beta-Carbolines; Trans-cinnamides; DNA intercalation; Topoisomerase I; Anticancer activity
Funding
- Council of Scientific and Industrial Research (CSIR), New Delhi (India) [CSC0301]
- University Grant Commission (UGC), Delhi
- SERB, DST, Govt. of India [YSS-2015-001709]
- DoP, Ministry of Chemicals & Fertilizers, Govt. of India, New Delhi
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A series of new C3-trans-cinnamide linked beta-carboline conjugates has been synthesized by coupling between various beta-carboline amines and substituted cinnamic acids. Evaluation of their anti-proliferative activity against a panel of selected human cancer cell lines such as A549 (lung cancer), MCF-7 (breast cancer), B16 (melanoma), HeLa (cervical cancer) and a normal cell line NIH3T3 (mouse embryonic fibroblast cell line), suggested that the newly designed conjugates are considerably active against all the tested cancer cell lines with IC50 values 13-45 nM. Moreover, the conjugates 8v and 8x were the most active against MCF-7 cells (14.05 nM and 13.84 nM respectively) and also even potent on other cell lines tested. Further, detailed investigations such as cell cycle analysis, apoptosis induction study, topoisomerase I inhibition assay, DNA binding affinity and docking studies revealed that these new conjugates are DNA interactive topoisomerase I inhibitors.
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