Synthesis and biological evaluation of heterocyclic analogues of pregnenolone as novel anti-osteoporotic agents
| Autor: | Ibadur R. Siddiqui, Krishna Bhan Singh, Divya Singh, Reena Rai, Kapil Dev, Saransh Wales Maurya, Rakesh Maurya |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Stereochemistry Clinical Biochemistry Pharmaceutical Science Bone matrix Biochemistry Bone morphogenetic protein 2 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Heterocyclic Compounds Drug Discovery medicine Humans Molecular Biology Biological evaluation Messenger RNA Chemistry Organic Chemistry Limiting Increased alp 030104 developmental biology Pregnenolone 030220 oncology & carcinogenesis Osteoporosis Molecular Medicine Acyl group medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 27:1390-1396 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2017.02.004 |
| Popis: | The structural modifications of pregnenolone have been described via the introduction of heterocyclic moieties at C-17 position by limiting the acyl group. Novel heterocyclic analogues of pregnenolone have been synthesized by using Friedlander and Claisen-Schmidt reactions, and the synthesized compounds were evaluated for their osteogenic activity. Among the synthesized derivatives, four compounds showed significantly increased ALP activity. Among all four active compounds, the novel compound 3a has shown significant bone matrix mineralization and mRNA expressions of osteogenic marker genes, BMP2, RUNX-2 and OCN at 1pM concentration. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect