Synthesis and biological evaluation of simplified analogs of lophocladine B as potential antitumor agents

In this study, two series of simplified isoquinolines deriving from lophocladine B were synthesized and evaluated for their antitumor activity. Suzuki-Miyaura and Sharpelss-Fokin reactions were employed to synthesize 26 compounds. Two compounds ( 25 and 27 ) showed to be cytotoxic with IC 50 values...

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Veröffentlicht in:	Medicinal chemistry research 2016-12, Vol.25 (12), p.2959-2964
Hauptverfasser:	Theeramunkong, Sewan, Vajragupta, Opa, Mudjupa, Chawannuch
Format:	Artikel
Sprache:	eng
Schlagworte:	Anticancer properties Antitumor activity Antitumor agents Apoptosis Biochemistry Biomedical and Life Sciences Biomedicine Cancer Cell Biology Cervical cancer Cervix Chemical reactions Chemical synthesis Cytotoxicity Liver cancer Original Research Pharmacology/Toxicology Toxicity
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Zusammenfassung:	In this study, two series of simplified isoquinolines deriving from lophocladine B were synthesized and evaluated for their antitumor activity. Suzuki-Miyaura and Sharpelss-Fokin reactions were employed to synthesize 26 compounds. Two compounds ( 25 and 27 ) showed to be cytotoxic with IC 50 values of 10 µM on hepatic cancer cells and 13 µM on cervical cancer cells, respectively. Further studies on their mechanism of action showed that compound 27 mediated cytotoxicity through apoptosis induction.
ISSN:	1054-2523 1554-8120
DOI:	10.1007/s00044-016-1717-5