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ABSTRACT
We have developed an efficient and straightforward methodology for the synthesis of novel tanshinone-substituted bis(indolyl/pyrrolyl)methane scaffolds 3 through TsOH catalysis-enabled addition of indoles or pyrroles 1 with tanshinones 2 based on molecular hybridization strategy. Products were smoothly obtained in good yields (up to 81% yield). This protocol also represents the first construction of tanshinone skeleton-fused bis(indolyl/pyrrolyl)methane scaffolds, thus leading to new knowledge in the fields of both molecular complexity and diversity-oriented synthesis and the lead compound discovery. Furthermore, their biological activities against human leukemia cells K562, human prostate cancer cells PC-3, and human lung cancer cells A549 have been preliminarily demonstrated by in vitro assays. The results demonstrated that most of these compounds 3 obtained by this protocol showed comparable activity to the positive control of cisplatin.
GRAPHICAL ABSTRACT
Acknowledgments
We are grateful for the financial support from the National Natural Science Foundations of China (No. 81660576, No. 81560563, No. 81760625 and No. 81603390); Excellent creative talents of guizhou province (Qian Jiao He KY Zi [(2015)491] and Qian Ke He Zi [2015]4032, [2017]5609); Guizhou Chinese medicine and pharmaceutical engineering professional degree graduate student workstation (JYSZ [2014]002); Project of Guizhou province (Qian Ke He Zi ([2016]5623 and [2015]4010) and Major project of the graduate student education teaching reform (Qian Jiao Yan He JG Zi)[2016]06.
