Vandresen Fábio, Falzirolli Hugo, Almeida Batista Sabrina A, da Silva-Giardini Ana Paula B, de Oliveira Diogo N, Catharino Rodrigo R, Ruiz Ana Lúcia T G, de Carvalho João E, Foglio Mary Ann, da Silva Cleuza Conceição
Departamento de Química, Centro de Ciências Exatas, Universidade Estadual de Maringá, Av. Colombo, 5790, CEP 87020-900, Maringá, PR, Brazil.
Departamento de Química, Centro de Ciências Exatas, Universidade Estadual de Maringá, Av. Colombo, 5790, CEP 87020-900, Maringá, PR, Brazil.
Eur J Med Chem. 2014 May 22;79:110-6. doi: 10.1016/j.ejmech.2014.03.086. Epub 2014 Apr 1.
In an attempt to develop potent and selective antitumor agents, a series of novel thiosemicarbazones derived from a natural monoterpene R-(+)-limonene was synthesized and their antitumor activity was evaluated. Overall, the majority of tested compounds exhibited considerable inhibitory effects on the growth of a wide range of cancer cell lines. Almost all of tested thiosemicarbazones were especially sensitive to prostate cells (PC-3). Derivatives 5, 6, 8, 9, 10, 11 and 13 presented the most potent antitumor activity against PC-3 cells. These compounds showed lower value of GI50 (0.04-0.05 μM) than the reference drug paclitaxel, besides a high selectivity for the same cell line. The 4-fluorobenzaldehyde derivative 10 was the most selective compound for prostate cells, while 2-hydroxybenzaldehyde derivative 8 was the most active compound, with potent antitumor activity against all tested cell lines.
为了开发高效且具有选择性的抗肿瘤药物，合成了一系列源自天然单萜R-(+)-柠檬烯的新型硫代氨基脲，并评估了它们的抗肿瘤活性。总体而言，大多数测试化合物对多种癌细胞系的生长表现出相当大的抑制作用。几乎所有测试的硫代氨基脲对前列腺细胞（PC-3）都特别敏感。衍生物5、6、8、9、10、11和13对PC-3细胞呈现出最强的抗肿瘤活性。这些化合物除了对同一细胞系具有高选择性外，其GI50值（0.04 - 0.05 μM）比参考药物紫杉醇还低。4-氟苯甲醛衍生物10是对前列腺细胞最具选择性的化合物，而2-羟基苯甲醛衍生物8是最具活性的化合物，对所有测试细胞系都具有强大的抗肿瘤活性。
