Concise Synthesis and Biological Evaluation of the Pyrrolo[4,3,2-<i>de</i>]quinoline Core of the Lymphostin Family
The efficient synthesis of the pyrrolo[4,3,2-<i>de</i>]quinoline core of the lymphostin family (compound <b>1</b>) has been accomplished in 7 steps and 18.6% overall yield, providing an efficient method for the total synthesis and structural modification of the lymphostin family. Compound <b>1</b> showed potent inhibitory activities against PI3K/mTOR in the nanomolar range and activity against human colorectal cancer cell lines comparable to that of oxaliplatin, which could be recognized as a novel lead compound for cancer therapy.
Authors
- Peng Cheng (ORCID: https://orcid.org/0000-0002-9797-6944)
- Yuqi Gao (ORCID: https://orcid.org/0009-0000-8501-0483)
- Lechao Cui
- Jiwei Xu (ORCID: https://orcid.org/0000-0002-2423-8123)
- Jiaojiao Yang (ORCID: https://orcid.org/0000-0002-8611-4089)
- Haojie Guo
- Xinyuan Zhang (ORCID: https://orcid.org/0000-0003-0388-2240)
- Tingting Liu (ORCID: https://orcid.org/0000-0002-5144-5179)
- Hongmin Li (ORCID: https://orcid.org/0009-0003-2739-2374)
- Jin Peng (ORCID: https://orcid.org/0000-0003-3410-6228)
- Jian Ning
- Chunjuan Tian
Institutions
- Academy of Medical Sciences (GB)
- Johns Hopkins University (US)
- Johns Hopkins Medicine (US)
- Qilu Normal University (CN)
- Shandong Provincial QianFoShan Hospital (CN)
- Shandong First Medical University (CN)
Publication Details
- Journal
- The Journal of Organic Chemistry
- Published
- 2024-10-23
- DOI
- https://doi.org/10.1021/acs.joc.4c02038
- Citations
- 1
- Primary Topic
- Synthesis and pharmacology of benzodiazepine derivatives
- Type
- article
- Field-Weighted Citation Impact
- 0.25
Funders
- Department of Education of Shandong Province
- National Natural Science Foundation of China