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1.
J Asian Nat Prod Res ; 21(7): 633-651, 2019 Jul.
Article in English | MEDLINE | ID: mdl-29733221

ABSTRACT

Using the techniques of computer-aided drug design, the docking of survivin and known active small molecules was simulated and then the key amino acid residue fragments of the target protein were analyzed. It led to the discovery of active groups capable of binding to the critical sites. Through the use of the natural product, oleanolic acid, as a lead compound, the introduction of the active groups onto the A-ring, and the modification of the carboxyl group at the C-28 position using esterification or amidation, 20 new oleanolic acid derivatives had been designed and synthesized. HepG2 and SGC-7901 cells were used to screen the antitumor activity through the standard MTT method. The compounds, II3, III5 and IV4, exhibited more potent cytotoxicity than positive drugs. Western blot experiment demonstrated that compound II3 can effectively inhibit the proliferation of HepG2 cells.


Subject(s)
Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Oleanolic Acid/chemical synthesis , Oleanolic Acid/pharmacology , Apoptosis/drug effects , Caspase Inhibitors/chemical synthesis , Caspase Inhibitors/pharmacology , Cell Line, Tumor , Cell Proliferation/drug effects , Drug Design , Drug Screening Assays, Antitumor , Hep G2 Cells , Humans , Molecular Docking Simulation , Molecular Structure , Oleanolic Acid/analogs & derivatives , Structure-Activity Relationship
2.
Quintessence Int ; 38(3): 253-9, 2007 Mar.
Article in English | MEDLINE | ID: mdl-17334004

ABSTRACT

Central giant cell granuloma is a relatively uncommon benign bony lesion of a variably aggressive nature. This paper presents the case of a 7-year-old boy with central giant cell granuloma in the anterior mandible. In children with mixed dentition, a pathologic lesion could be the underlying cause of regular tooth mobility and exfoliation of primary teeth and can easily be overlooked, especially in cases that are not accompanied by an obvious bony expansion. The clinician needs to be aware of possible oral pathology when tooth mobility and displacement are present, and central giant cell granuloma should be considered in the differential diagnosis for children with maligned and mobile teeth.


Subject(s)
Granuloma, Giant Cell/pathology , Mandibular Diseases/pathology , Child , Diagnosis, Differential , Granuloma, Giant Cell/complications , Humans , Male , Mandibular Diseases/complications , Tooth Mobility/etiology
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