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1.
Bioorg Med Chem Lett ; 27(15): 3450-3453, 2017 08 01.
Article in English | MEDLINE | ID: mdl-28587825

ABSTRACT

A series of 3-carbamate and 29-ester celastrol derivatives (compounds 1-26) were designed and synthesized. These analogues were evaluated for their cytotoxic activities against several cancer cell lines. Cytotoxicity data revealed that the properties of substituents and substitution position had important influence on cytotoxic activity. Modification of C-3 hydroxyl with size-limited groups did not reduce the activity obviously. The introduction of polarity group like piperazine could improve the solubility. Compound 23 was chosen to further evaluate anti-tumor efficacy in vivo. It showed higher inhibition rate and better safety than celastrol during in vivo experiment by intragastric administration. The preliminary antitumor studies of compound 23in vivo showed that it might be promising for the development of new antitumor agents.


Subject(s)
Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Triterpenes/chemistry , Triterpenes/pharmacology , A549 Cells , Animals , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/therapeutic use , Cell Line, Tumor , Cell Survival/drug effects , Drug Design , Drug Screening Assays, Antitumor , Esterification , Humans , Mice, Nude , Neoplasms/drug therapy , Neoplasms/pathology , Pentacyclic Triterpenes , Structure-Activity Relationship , Triterpenes/chemical synthesis , Triterpenes/therapeutic use
2.
Chem Biodivers ; 9(12): 2754-60, 2012 Dec.
Article in English | MEDLINE | ID: mdl-23255445

ABSTRACT

Two new labdane diterpenoids, namely hedycoronals A and B (1 and 2, resp.), were isolated from the rhizomes of Hedychium coronarium, together with eight known diterpenoids, 4-11, and a known diarylheptanoid, 3. The structures of 1 and 2 were established by detailed interpretation of their 1D- and 2D-NMR spectra and HR-ESI-MS data. Inhibitory activities against human umbilical vein endothelial cells (HUMECs) proliferation and cytotoxic activities against four cancer cell lines were assessed for all the isolates. Most of these metabolites showed moderate or potent cytotoxic activities against four cancer cell lines. Moreover, compounds 3 and 8 exhibited promising inhibitory activities against HUMECs with the IC(50) values of 6.4 to 3.3 µM.


Subject(s)
Diarylheptanoids/chemistry , Diterpenes/chemistry , Zingiberaceae/chemistry , Angiogenesis Inhibitors/chemistry , Angiogenesis Inhibitors/isolation & purification , Angiogenesis Inhibitors/pharmacology , Cell Line, Tumor , Cell Proliferation/drug effects , Diarylheptanoids/pharmacology , Diarylheptanoids/toxicity , Diterpenes/pharmacology , Diterpenes/toxicity , Human Umbilical Vein Endothelial Cells , Humans , Magnetic Resonance Spectroscopy , Molecular Conformation , Rhizome/chemistry
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