Bhornrawin AkkachairinWarabhorn RodphonOnrapak ReamtongMathirut MungthinJumreang TummatornCharnsak ThongsornkleebSomsak RuchirawatSouth Carolina Commission on Higher EducationChulabhorn Research InstituteMahidol UniversityPhramongkutklao College of Medicine2020-03-262020-03-262020-05-01Bioorganic Chemistry. Vol.98, (2020)10902120004520682-s2.0-85081222736https://repository.li.mahidol.ac.th/handle/20.500.14594/53560© 2020 Elsevier Inc. 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.Mahidol UniversityBiochemistry, Genetics and Molecular BiologyChemistryPharmacology, Toxicology and PharmaceuticsArticleSCOPUS10.1016/j.bioorg.2020.103732