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Tinghan Li
China Pharmaceutical University
5Publications
3H-index
16Citations
Publications 5
Newest
#1Jubo Wang (CPU: China Pharmaceutical University)H-Index: 6
#2Tinghan Li (CPU: China Pharmaceutical University)H-Index: 3
Last.Jinlei Bian (CAS: Chinese Academy of Sciences)
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Abstract Wogonin, a natural product isolated from the plant Scutellaria baicalensis , has been shown to be a potent and selective inhibitor of CDK9. With the purpose of investigating the activity and selectivity of this chemical scaffold, several series of wogonin derivatives were prepared and screened for CDK9 inhibition and cellular antiproliferative activity. Among these compounds, the drug-like compound 51 showed potent activity against CDK9 (IC 50 = 19.9 nM) and MV4-11 cell growth (IC 50 = ...
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#1Tinghan LiH-Index: 3
#2Tianwei WengH-Index: 3
Last.Zhiyu LiH-Index: 22
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A scalable and practical route to wogonin, a bioactive natural product with multiple pharmacological activities which is currently under phase I/II clinical studies, is described. Wogonin was obtained via a four-step process starting from commercially available chrysin and including the Elbs oxidation, benzylation, methylation, and the final debenzylation. The whole procedure gives the target product in a 38% overall yield with >99% purity. Key steps in this process including oxidation and methy...
1 CitationsSource
#1Jinlei Bian (CPU: China Pharmaceutical University)H-Index: 10
#2Tinghan Li (CPU: China Pharmaceutical University)H-Index: 3
Last.Zhiyu Li (CPU: China Pharmaceutical University)H-Index: 22
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Abstract A novel series of 49 wogonin derivatives were synthesized by introducing group at 7-, 8- or B ring of wogonin. The cytotoxic activities against HepG2, A549 and BCG-823 cancer cell lines were also investigated in vitro . Several of them showed obvious cytotoxic activities and compound 3h possessed the highest potency against HepG2, A549, and BCG-823 with IC 50 values of 1.07 μM, 1.74 μM and 0.98 μM, respectively. A quantitative structure-activity relationship (QSAR) study of these synthe...
5 CitationsSource
#1Tinghan LiH-Index: 3
#2Tianwei WengH-Index: 3
Last.Zhiyu LiH-Index: 22
view all 6 authors...
Deregulation of the cell cycle is a common feature in human cancer. The inhibition of cyclin-dependent kinases (CDKs), which play a crucial role in control of the cell cycle, has always been one of the most promising areas in cancer chemotherapy. This review first summarizes the biology of CDKs and then focuses on the recent advances in both broad-range and selective CDK inhibitors during the last 5 years. The design rationale, structural optimization and structure–activity relationships analysi...
4 CitationsSource
#1Minzan ZuoH-Index: 2
#2Xi XuH-Index: 5
Last.Zhiyu LiH-Index: 22
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Although prostate cancer can initially respond to androgen deprivation therapy, it will inevitably relapse and switch to a castration-resistant state. The progress in understanding the mechanism of castration-resistant prostate cancer (CRPC) has led to the evolution of novel agents, including sipuleucel-T as an immunomodulant agent, enzalutamide as an androgen receptor antagonist, docetaxel as a chemotherapeutic agent and radium-223 as a radiopharmaceutical agent. In this review, we discuss the ...
6 CitationsSource
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