Journal
BIOORGANIC CHEMISTRY
Volume 98, Issue -, Pages -Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2020.103732
Keywords
Neocryptolepine; Antiplasmodial; Anticancer; Indoloquinoline; Azide; Carbocycle-fused quinolines
Funding
- Chulabhorn Research Institute, Mahidol University
- Center of Excellence on Environmental Health and Toxicology, Science & Technology Postgraduate Education and Research Development Office (PERDO), Ministry of Education Education
- Thailand Research Fund through the Royal Golden Jubilee (RGJ) Ph.D. Program [PHD/0181/2559]
- Thailand Research Fund [RSA6080085]
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This study reported the discovery of novel compounds containing five-membered ring fused quinoline core structures as anticancer and antimalarial agents. Two libraries containing these core structures, neocryptolepines and carbocycle-fused quinolines, were prepared and evaluated. Compound 3h was found to be much more potent than other analogs against cancer cell lines with high selectivity. Meanwhile, carbocycle-fused quinolines 5h and 5s showed moderate anticancer properties but much less cytotoxicity to normal cell than doxorubicin. In addition, compound 3h also showed much lower cytotoxic against human normal kidney cell line compared to doxorubicin standard. However, only compounds 3s and 3p provided acceptable results for antimalarial activities.
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