División de Ciencias de la Salud, Universidad de Quintana Roo. Av., Chetumal, Quintana Roo, México.
Facultad de Química, Universidad Autónoma de Yucatán, Mérida, Yucatán, México.
Nat Prod Res. 2022 Sep;36(18):4714-4718. doi: 10.1080/14786419.2021.2001809. Epub 2021 Nov 7.
A series of 15 novel 1,3-thiazole amide derivatives of the pentacyclic triterpene Ochraceolide A () was synthesized, characterized, and evaluated against three human cancer cell lines (MCF-7, MDA-MB-231 and SiHa) and a normal cell line (Vero). Synthetic derivatives were obtained by acylation of the 2-aminothiazole triterpene , previously reported. Remarkably, the 5-nitrofuramide derivative () showed better cytotoxic and antiproliferative activity than compound and the other derivatives against the three cancer cell lines with CC and IC values of 1.6-12.7 µM. Furthermore, butyramide derivative () was approximately 25 times more selective than , as well as 3.4 times more selective than Docetaxel, against SiHa cells in the cytotoxic assay, while the phenyl amide derivatives were inactive against the three cancer cell lines.
合成了一系列新型 1,3-噻唑酰胺衍生物 pentacyclic triterpene Ochraceolide A ()，并对其进行了表征，同时评估了它们对三种人癌细胞系（MCF-7、MDA-MB-231 和 SiHa）和一种正常细胞系（Vero）的抑制活性。通过对之前报道的 2-氨基噻唑三萜进行酰化，得到了合成衍生物。值得注意的是，5-硝基呋喃酰胺衍生物 () 对三种癌细胞系的细胞毒性和增殖抑制活性均优于化合物 和其他衍生物，其 CC50 和 IC50 值分别为 1.6-12.7 μM。此外，在细胞毒性试验中，丁酰胺衍生物 () 对 SiHa 细胞的选择性比 高约 25 倍，比多西他赛高 3.4 倍，而苯甲酰胺衍生物对三种癌细胞系均无活性。
