2. Academic Validation
  3. Synthesis of neocryptolepines and carbocycle-fused quinolines and evaluation of their anticancer and antiplasmodial activities

Synthesis of neocryptolepines and carbocycle-fused quinolines and evaluation of their anticancer and antiplasmodial activities

  • Bioorg Chem. 2020 May;98:103732. doi: 10.1016/j.bioorg.2020.103732.
Bhornrawin Akkachairin 1,  Warabhorn Rodphon 1,  Onrapak Reamtong 2,  Mathirut Mungthin 3,  Jumreang Tummatorn 4,  Charnsak Thongsornkleeb 5,  Somsak Ruchirawat 5
Affiliations

Affiliations

  • 1 Program on Chemical Biology, Chulabhorn Graduate Institute, Center of Excellence on Environmental Health and Toxicology, CHE, Ministry of Education, 54 Kamphaeng Phet 6, Laksi, Bangkok 10210, Thailand.
  • 2 Department of Molecular Tropical Medicine and Genetics, Faculty of Tropical Medicine, Mahidol University, Bangkok, Thailand.
  • 3 Department of Parasitology, Phramongkutklao College of Medicine, Ratchawithi Road, Bangkok 10400, Thailand.
  • 4 Program on Chemical Biology, Chulabhorn Graduate Institute, Center of Excellence on Environmental Health and Toxicology, CHE, Ministry of Education, 54 Kamphaeng Phet 6, Laksi, Bangkok 10210, Thailand; Chulabhorn Research Institute, 54 Kamphaeng Phet 6, Laksi, Bangkok 10210, Thailand. Electronic address: [email protected].
  • 5 Program on Chemical Biology, Chulabhorn Graduate Institute, Center of Excellence on Environmental Health and Toxicology, CHE, Ministry of Education, 54 Kamphaeng Phet 6, Laksi, Bangkok 10210, Thailand; Chulabhorn Research Institute, 54 Kamphaeng Phet 6, Laksi, Bangkok 10210, Thailand.
PMID: 32171989 DOI: 10.1016/j.bioorg.2020.103732
Abstract

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.

Keywords

Anticancer; Antiplasmodial; Azide; Carbocycle-fused quinolines; Indoloquinoline; Neocryptolepine.

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