Populene D Analogues: Design, Concise Synthesis and Antiproliferative Activity

Molecules

Kachi R. Kishore Kumar Reddy²  Giovanna B. Longato¹  João E. de Carvalho¹  Ana L. T. G. Ruiz¹ 

[1]Divisão de Farmacologia e Toxicologia, Centro Pluridisciplinar de Pesquisas Químicas, Biológicas e Agrícolas (CPQBA), UNICAMP, CP6171, Campinas 13083-970, SP, Brazil

[2]Instituto de Química, Universidade de São Paulo, Av. Prof. Lineu Prestes, 748, CP 26077, CEP São Paulo 05513-970, SP, Brazil

关键词: osochromene;    pyrans;    Prins cyclization;    iodine;    antiproliferative;    cancer;   

DOI  :  10.3390/molecules17089621

来源: mdpi

【 摘 要 】

An efficient and concise synthesis of nine populene D analogues was performed using an iodine-catalyzed Prins cyclization as the key transformation. The antiproliferative activity of these new pyrans against several cancer cell lines was then investigated. Among them, an isochromene with moderate activity (mean logGI₅₀ = 0.91) was found. Additionally, compounds with selectivity toward the tumor cell lines NCI-ADR/RES, OVCAR-3, and HT29 were discovered.

【 授权许可】

CC BY   
© 2012 by the authors; licensee MDPI, Basel, Switzerland.