肿瘤耐药是当今化疗中最常见和棘手的问题，找寻相应的抗多药耐药肿瘤的有效药物具有十分重要的意义。本项目以兼具细胞毒活性（对耐药肿瘤有效）和逆转肿瘤多药耐药活性的片螺素为先导，提取其核心活性单元，与吡咯并三嗪优势骨架相结合，分别从这两个方向开发新型抗多药耐药肿瘤药物。该结构改造简化了复杂的多环结构，引入了新的可修饰位点，以平衡化合物的生物活性和药代动力学性质，有望从根本上解决片螺素成药性差的难题，具有较高的研究意义与应用价值。

Multidrug resistance is one of the main challenge for clinical chemotherapy treatment on tumors. Therefore, continuing efforts in discovering novel antitumor drugs that could overcome multidrug resistance is urgent. Lamellarins possess promising bioactivities of both cytotoxicity against multidrug resistant tumor cell lines and reversing multidrug resistant phenotype, and thus were selected as lead compounds for further antitumor drug development. We embark on designing novel analogues of Lamellarins through scaffold hopping with pyrrolo[2, 1-f][1,2,4]triazine on the basis of their core unit. This strategy is involved with cutting the original polycyclic nucleus and introducing new modified sites to balance their antitumor activities and pharmacokinetic profiles, which is of great scientific research value.