150614-67-8Relevant articles and documents
Design, synthesis and antitumour and anti-angiogenesis evaluation of 22 moscatilin derivatives
Guan, Li,Zhou, Junting,Lin, Qinghua,Zhu, Huilin,Liu, Wenyuan,Liu, Baolin,Zhang, Yanbo,Zhang, Jie,Gao, Jing,Feng, Feng,Qu, Wei
, p. 2657 - 2665 (2019/05/01)
Two series of moscatilin derivatives were designed, synthesized and evaluated as anti-tumor and anti-angiogenesis agents. Most of these compounds showed moderate-to-obvious cytotoxicity against five cancer cell lines (A549, HepG2, MDA-MB-231, MKN-45, HCT116). Among these cell lines, compounds had obvious effects on HCT116. Especially for 8Ae, the IC50 was low to 0.25 μM. 8Ae can inhibit the viability and induce the apoptosis of HCT116 cells but exhibit no cytotoxic activity in noncancerous NCM460 colon cells. 8Ae can also arrest the G2/M cell cycle in HCT116 cells by inhibiting the α-tubulin expression. Zebrafish bioassay-guided screen showed the 22 moscatilin derivatives had potent anti-angiogenic activities and compound 8Ae had better activities than positive compound. Molecular docking indicated 8Ae interacted with tubulin at the affinity of ?7.2 Kcal/mol. In conclusion, compound 8Ae was a potential antitumor and anti-angiogenesis candidate for further development.
Synthesis and evaluation of neuroprotective 4-O-substituted chrysotoxine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease
Guan, Li,Hao, Yanfeng,Chen, Lei,Wei, Meng-Lin,Jiang, Qin,Liu, Wen-Yuan,Zhang, Yan-Bo,Zhang, Jie,Feng, Feng,Qu, Wei
, p. 22827 - 22838 (2016/03/12)
A series of 4-O-substituted chrysotoxine (CTX) derivatives were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer's disease (AD). In vitro assays indicated that four ring substituted compounds (2a, 2b, 3i and 3j)
NOVEL HETEROCYCLIC COMPOUNDS AS HSP90-INHIBITORS
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Page/Page column 314, (2008/06/13)
Novel heterocyclic compounds are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agent. Method of synthesis and use of such compounds are also described.