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

Bhornrawin Akkachairin, Warabhorn Rodphon, Onrapak Reamtong, Mathirut Mungthin, Jumreang Tummatorn, Charnsak Thongsornkleeb, Somsak Ruchirawat

Bioorganic chemistry 2020 May

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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. Copyright © 2020 Elsevier Inc. All rights reserved.

Citation

Bhornrawin Akkachairin, Warabhorn Rodphon, Onrapak Reamtong, Mathirut Mungthin, Jumreang Tummatorn, Charnsak Thongsornkleeb, Somsak Ruchirawat. Synthesis of neocryptolepines and carbocycle-fused quinolines and evaluation of their anticancer and antiplasmodial activities. Bioorganic chemistry. 2020 May;98:103732