Rajabi, MehdiMousa, Shaker A.2024-03-252024-03-252018-02-24Rajabi, M. vd. (2018). ''Synthesis of new analogs of tetraiodothyroacetic acid (tetrac) as novel angiogenesis inhibitors for treatment of cancer''. Bioorganic and Medicinal Chemistry Letters, 28(7), 1223-1227.0960-894Xhttps://www.sciencedirect.com/science/article/pii/S0960894X18301501https://hdl.handle.net/11452/40618In the angiogenesis process, integrins, which are members of a family of cell surface transmembrane receptors, play a critical role particularly in blood vessel formation and the local release of vascular growth factors. Thyroid hormones such as L-thyroxine (T-4) and 3,5,30-triiodo-L-thyronine (T-3) promote angiogenesis and tumor cell proliferation via integrin alpha v beta 3 receptor. At or near an arginine-glycine-aspartate (RGD) recognition site on the binding pocket of integrin avb3, tetraiodothyroacetic acid (tetrac, a deaminated derivative of T-4) is a thyrointegrin receptor antagonist and blocks the actions of T-3 and T-4 as well as different growth factors-mediated angiogenesis. In this study, we synthesized novel tetrac analogs by modifying the phenolic moiety of tetrac and tested them for their anti-angiogenesis activity using a Matrigel plug model for angiogenesis in mice. Pharmacological activity results showed that tetrac can accommodate numerous modifications and maintain its anti-angiogenesis activity.eninfo:eu-repo/semantics/closedAccessPharmacology & pharmacyChemistryAngiogenesisThyroid hormonesTetraiodothyroacetic acidTetracIntegrinL-thyeoxineTumorThalidomideGrowthMetabolitesIntegrinsAngiogenesis inhibitorsAnimalsAntineoplastic agentsCell proliferationDisease models, animalDose-response relationship, drugDrug screening assays, antitumorFemaleHumansMiceMice, inbred C57BLMolecular structureNeoplasmsNeoplasms, experimentalNeovascularization, pathologicStructure-activity relationshipThyroxineArticle0004280924000132-s2.0-850428736431223122728729519736https://doi.org/10.1016/j.bmcl.2018.02.045Chemistry, medicinalChemistry, organicIntegrin; Thyroid Hormones; Nano-Diamino-TetracAngiogenesis inhibitorAntineoplastic agentTetraiodothyroacetic acidTetraiodothyroacetic acid derivativeThalidomideUnclassified drugAngiogenesis inhibitorAntineoplastic agentTetraiodothyroacetic acidThyroxineAnimal experimentAnimal modelAntiangiogenic activityArticleCancer chemotherapyChemical modificationControlled studyDrug solubilityDrug synthesisFemaleIn vivo studyLiquid chromatographyMass spectrometryMouseMouse modelNonhumanStructure activity relationAnalogs and derivativesAnimalC57BL mouseCell proliferationChemical structureChemistryDisease modelDose responseDrug effectDrug screeningExperimental neoplasmHumanNeoplasmNeovascularization (pathology)PathologySynthesis1464-3405