Resveratrol, a natural compound known especially for its antioxidant properties and protective action, opens the door for both it and its structural derivatives to be considered not only as chemopreventive but also as cancer chemotherapeutic agents. Due to the pharmacokinetic problems of resveratrol that demonstrate its poor bioavailability, the study of new derivatives is of interest. Thus, in this work (E)-stilbenes derived directly from resveratrol and other cyclic analogues containing the benzofuran or indole nucleus have been synthesized. The synthesized compounds have been evaluated for their ability to affect tumor growth in vitro. Compounds 2, 3, 4 and 5 have shown cytotoxicity in human colon cancer (HT-29) and human pancreatic adenocarcinoma cells (MIA PaCa-2) higher than those of (E)-resveratrol. The indolic derivative 13, a cyclic analog of resveratrol, has shown in vitro cytotoxic activity 8 times higher than resveratrol against HT-29 cancer cells. The cyclic derivatives 8, 9 and 12 showed a high inhibition of cell growth in HCT-116 (KRas mutant) at 20 μM, while 13 shows moderate antiangiogenesis activity at 10 μM.

白藜芦醇是一种以其抗氧化特性和保护作用而闻名的天然化合物，它为其及其结构衍生物打开了大门，使其不仅被视为化学预防剂，而且被视为癌症化学治疗剂。由于白藜芦醇的药代动力学问题表明其生物利用度差，因此对新衍生物的研究引起了人们的兴趣。因此，在这项工作中，已经合成了直接衍生自白藜芦醇和其他含有苯并呋喃或吲哚核的环状类似物的 ( E )-二苯乙烯。已经评估了合成化合物在体外影响肿瘤生长的能力。化合物2 , 3 , 4和5已显示在人结肠癌 (HT-29) 和人胰腺癌细胞 (MIA PaCa-2) 中的细胞毒性高于 ( E )-白藜芦醇。吲哚衍生物13是白藜芦醇的一种环状类似物，在体外显示出对 HT-29 癌细胞的细胞毒活性比白藜芦醇高 8 倍。环状衍生物8、9和12在20 μM 时显示出对 HCT-116（KRas 突变体）细胞生长的高度抑制，而13在10 μM 时显示出中等的抗血管生成活性。