Search results for "bisphosphonates."
showing 10 items of 66 documents
Design, synthesis, and biological evaluation of novel aminobisphosphonates possessing an in vivo antitumor activity through a gammadelta-T lymphocyte…
2008
A small series of aminobisphosphonates (N-BPs) structurally related to zoledronic acid was synthesized with the aim of improving activity toward activation of human gammadelta T cells and in turn their in vivo antitumor activity. The absence of the 1-OH moiety, together with the position and the different basicity of the nitrogen, appears crucial for antitumor activity. In comparison to zoledronic acid, compound 6a shows a greater ability to activate gammadelta T cells expression (100 times more) and a proapoptotic effect that is better than zoledronic acid. The potent activation of gammadelta T cells, in addition to evidence of the in vivo antitumor activity of 6a, suggests it may be a new…
Medication-Related Osteonecrosis of Jaws (MRONJ) Prevention and Diagnosis: Italian Consensus Update 2020
2020
The Medication-Related Osteonecrosis of Jaws (MRONJ) diagnosis process and its prevention play a role of great and rising importance, not only on the Quality of Life (QoL) of patients, but also on the decision-making process by the majority of dentists and oral surgeons involved in MRONJ prevention (primary and secondary). The present paper reports the update of the conclusions from the Consensus Conference—held at the Symposium of the Italian Society of Oral Pathology and Medicine (SIPMO) (20 October 2018, Ancona, Italy)—after the newest recommendations (2020) on MRONJ were published by two scientific societies (Italian Societies of Maxillofacial Surgery and Oral Pathology and Medicine, SI…
Synthesis of N-methyl alkylaminomethane-1,1-diphosphonic acids and evaluation of their complex-formation abilities towards copper(II)
2015
Abstract A series of N -methyl alkylaminomethane-1,1-diphosphonic acids ( 3a – g ) with a common tertiary nitrogen atom (CH 3 –N–R) bearing linear or branched alkyl, cycloheptyl or phenylalkyl R substituents was synthesized in the reaction of diethylphosphonate with triethyl orthoformate and secondary amine followed by hydrolysis, and by the Eschweiler–Clarke methylation of the alkylaminomethane-1,1-diphosphonic acids with formic acid and formaldehyde. Complex-formation abilities of 3a – g towards copper(II) in solution were studied by means of pH-potentiometry, ESI-MS spectrometry, UV–Vis and EPR methods. Evaluation of stability constants for the Cu(II) complexes of 3a – g has revealed the…
Herbicidally Active Derivatives of Aminomethylenebis-Phosphonic Acid-Mode of Action and Structure - Activity Relationship
1996
Abstract: (N-pyridylamino)methylenebisphosphonates exhibit strong herbicidal activity which may be reversed by supplementation of the growth media with aromatic amino acids. They appeare to be the inhibitors of aromatic amino acids biosynthesis acting as inhibitors of DAHP synthase the first enzyme of shikimate pathway. Over 40 analogues of these acids were synthesized in order to determine the structure-activity relationship.
Herbicidal Derivatives of Aminomethylenebisphosphonic Acid. Part IV. Hydroxyalkylidenebisphosphonates, Iminomethylenebisphosphonates and Ureidomethyl…
2000
Derivatives of aminomethylenebisphosphonic acids constitute a class of promising herbicides. Replacement of the amino group by hydroxyl, ureido, thioureido, or imino moieties leads to compounds of significant herbicidal properties. This indicates that protonated amino function is not a requirement for phytotoxic action of bisphosphonates.
Novel Radiolabeled Bisphosphonates for PET Diagnosis and Endoradiotherapy of Bone Metastases.
2017
Bone metastases, often a consequence of breast, prostate, and lung carcinomas, are characterized by an increased bone turnover, which can be visualized by positron emission tomography (PET), as well as single-photon emission computed tomography (SPECT). Bisphosphonate complexes of 99mTc are predominantly used as SPECT tracers. In contrast to SPECT, PET offers a higher spatial resolution and, owing to the 68Ge/68Ga generator, an analog to the established 99mTc generator exists. Complexation of Ga(III) requires the use of chelators. Therefore, DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid), NOTA (1,4,7-triazacyclododecane-1,4,7-triacetic acid), and their derivatives, are ofte…
Bone targeting compounds for radiotherapy and imaging: *Me(III)-DOTA conjugates of bisphosphonic acid, pamidronic acid and zoledronic acid
2016
Background Bisphosphonates have a high adsorption on calcified tissues and are commonly used in the treatment of bone disorder diseases. Conjugates of bisphosphonates with macrocyclic chelators open new possibilities in bone targeted radionuclide imaging and therapy. Subsequent to positron emission tomography (PET) examinations utilizing 68Ga-labelled analogues, endoradiotheraphy with 177Lu-labelled macrocyclic bisphosphonates may have a great potential in the treatment of painful skeletal metastases. Methods Based on the established pharmaceuticals pamidronate and zoledronate two new DOTA-α-OH-bisphosphonates, DOTAPAM and DOTAZOL(MM1.MZ) were successfully synthesized. The ligands were labe…
Evaluation of the inverse electron demand Diels-Alder reaction in rats using a scandium-44-labelled tetrazine for pretargeted PET imaging
2019
Background Pretargeted imaging allows the use of short-lived radionuclides when imaging the accumulation of slow clearing targeting agents such as antibodies. The biotin-(strept)avidin and the bispecific antibody-hapten interactions have been applied in clinical pretargeting studies; unfortunately, these systems led to immunogenic responses in patients. The inverse electron demand Diels-Alder (IEDDA) reaction between a radiolabelled tetrazine (Tz) and a trans-cyclooctene (TCO)-functionalized targeting vector is a promising alternative for clinical pretargeted imaging due to its fast reaction kinetics. This strategy was first applied in nuclear medicine using an 111In-labelled Tz to image TC…
Review and update on drugs related to the development of osteonecrosis of the jaw
2019
Conflict of interest Conclusions of the working group on “New drugs related to the de-velopment of osteonecrosis of the jaw”. Spanish Society of Cranio-mandibular Dysfunction and Orofacial Pain and Spanish Society of Oral Medicine SEDCYDO-SEMO joint International Meeting: 30th SEDCYDO annual meeting & 15th SEMO Congress. Bilbao (Spain); June, 2019. [EN] Background: Medication-related osteonecrosis of the jaw (MRONJ) is a rare, but serious adverse effect of cer-tain drugs, of which bisphosphonates are the most widely known. This pathology is also associated with other medications such as the biologic antiresorptive agent, denosumab and some antiangiogenics such as sunitinib, bevacizumab or a…
Improving adherence in osteoporosis: a new management algorithm for the patient with osteoporosis
2011
Introduction: Bisphosphonates are the first-choice treatment for osteoporosis. They effectively increase bone mineral density, reduce markers of bone resorption, and lower the incidence of new fractures in patients with osteoporosis-related fracture. However, the efficacy observed in clinical trials may not be realized in a real-life setting, partly due to poor adherence to therapy, with a significant worsening of clinical outcomes. Several issues contribute to poor adherence to osteoporosis medication, including inconvenient dosing regimens and concerns about possible adverse events. Although strategies to improve adherence have been investigated, new approaches are required. Areas covered…