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Diversity-oriented TsOH catalysis-enabled construction of tanshinone-substituted bis(indolyl/pyrrolyl)methanes and their biological evaluation for anticancer activities.
- Source :
-
Synthetic Communications . Dec2017, Vol. 47 Issue 24, p2378-2386. 9p. - Publication Year :
- 2017
-
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. [ABSTRACT FROM AUTHOR]
- Subjects :
- *ANTINEOPLASTIC agents
*PROSTATE cancer
*LEUKEMIA
*CISPLATIN
*PYRROLES
Subjects
Details
- Language :
- English
- ISSN :
- 00397911
- Volume :
- 47
- Issue :
- 24
- Database :
- Academic Search Index
- Journal :
- Synthetic Communications
- Publication Type :
- Academic Journal
- Accession number :
- 126511280
- Full Text :
- https://doi.org/10.1080/00397911.2017.1378359