Several derivatives of a series that share a thienoisoquinoline scaffold have demonstrated potent activity against cancer cell lines A549, HeLa, HCT-116, and MDA-MB-231 in the submicromolar concentration range. Structure-activity relationship (SAR) studies on a range of derivatives aided in identifying key pharmacophores in the lead compound. A series of compounds have been identified as the most promising with submicromolar IC₅₀ values against a lung cancer cell line (A549). Microscopy studies of cancer cells treated with the lead compound revealed that it causes mitotic arrest and disrupts microtubules. Further evaluation via an in vitro microtubule polymerization assay and competition studies indicate that the lead compound binds to tubulin via the colchicine site.

共享噻吩并异喹啉支架的一系列衍生物已在亚微摩尔浓度范围内显示出对癌细胞系 A549、HeLa、HCT-116 和 MDA-MB-231 的有效活性。对一系列衍生物的构效关系 (SAR) 研究有助于识别先导化合物中的关键药效​​团。一系列化合物已被确定为对肺癌细胞系 (A549)具有亚微摩尔 IC ₅₀值的最有希望的化合物。用先导化合物处理的癌细胞的显微镜研究表明，它会导致有丝分裂停滞并破坏微管。通过体外微管聚合测定和竞争研究的进一步评估表明，先导化合物通过秋水仙碱位点与微管蛋白结合。