title: Design and synthesis of dalbergin analogues and evaluation of anti-osteoporotic activity.
abstract: The chemical modifications of the hydroxyl group of dalbergin have been described via the introduction of cyclic amine, ester and amide groups. Among the twenty-three prepared novel analogues of dalbergin, compound 4d (EC502.3μM) showed significantly increased proliferation as assessed by alkaline phosphatase activity and mineralization in calvarial osteoblast cells in vitro. Compound 4d, at a dose of 1.0mg/kg body weight exhibited the significant osteoprotective effect. It showed a significant increase in osteogenic gene expression RunX2 (∼4fold), ALP (∼5fold), OCN (∼4fold) and COL1 (∼4fold) as compared to control group at the same dose in vivo assay.
authors.affiliation: Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
authors.forename: Padam
authors.initials: P
authors.lastname: Kumar
authors.affiliation: Academy of Scientific and Innovative Research, CSIR-Central Drug Research Institute, Lucknow 226031, India; Endocrinology Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
authors.forename: Priyanka
authors.initials: P
authors.lastname: Kushwaha
authors.affiliation: Endocrinology Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
authors.forename: Naseer
authors.initials: N
authors.lastname: Ahmad
authors.affiliation: Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, India; Department of Chemistry, University of Allahabad, Allahabad 211002, India.
authors.forename: Saransh Wales
authors.initials: SW
authors.lastname: Maurya
authors.affiliation: Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, India; Academy of Scientific and Innovative Research, CSIR-Central Drug Research Institute, Lucknow 226031, India.
authors.forename: Kapil
authors.initials: K
authors.lastname: Dev
authors.affiliation: Endocrinology Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
authors.forename: Vikram
authors.initials: V
authors.lastname: Khedgikar
authors.affiliation: Department of Chemistry, University of Allahabad, Allahabad 211002, India.
authors.forename: Ibadur Rahman
authors.initials: IR
authors.lastname: Siddiqui
authors.affiliation: Endocrinology Division, CSIR-Central Drug Research Institute, Lucknow 226031, India. Electronic address: ritu_trivedi@cdri.res.in.
authors.forename: Ritu
authors.initials: R
authors.lastname: Trivedi
authors.affiliation: Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, India; Academy of Scientific and Innovative Research, CSIR-Central Drug Research Institute, Lucknow 226031, India. Electronic address: mauryarakesh@rediffmail.com.
authors.forename: Rakesh
authors.initials: R
authors.lastname: Maurya
mesh_terms: D000818:Animals; D055396:Bone Morphogenetic Protein 2 / Q000378:metabolism; D002113:Calcification, Physiologic / Q000187:drug effects; D002478:Cells, Cultured; D003374:Coumarins / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use*; D015195:Drug Design; D005260:Female; D005786:Gene Expression Regulation / Q000187:drug effects; D006801:Humans; D008807:Mice, Inbred BALB C; D010006:Osteoblasts / Q000187:drug effects* / Q000378:metabolism / Q000473:pathology; D010012:Osteogenesis / Q000187:drug effects*; D015663:Osteoporosis, Postmenopausal / Q000188:drug therapy* / Q000235:genetics / Q000378:metabolism / Q000473:pathology; D012886:Skull / Q000166:cytology / Q000187:drug effects / Q000378:metabolism / Q000473:pathology
chemical_list: D055396:Bone Morphogenetic Protein 2; D003374:Coumarins; C000613895:dalbergin
keywords: Aminodalbergin; Dalbergin; Micro-CT; Post-menopausal osteoporosis; Ritter reaction