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Title: Modified Isoflavonoids: Design, Synthesis and Antiproliferative Activity 

Abstract: An antiproliferative natural pterocarpan was the starting point to design synthetic pterocarpanquinones. After a SAR study of these compounds in a panel of cancer cells, including some with MDR phenotype, LQB-118 was selected for in vivo experiments and presented anti-cancer (leukemia, prostate) and antileishmanial properties in mice. Additional SAR studies led to LQB-223, a 5-carba-11-aza-pterocarpan. This compound and some structural analogues presented potent antiproliferative effect in leukemia and mama cancer cell lines. New pterocarpans, 5-Carba-pterocarpans and 1-carba-isoflavanones were also synthesized and showed promising antiproliferative activity. The synthesis of these compounds and possible mechanisms of action will be discussed.

 

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  • BrazMedChem