ABSTRACT
In the light of recently disclosed crystallographic studies on migrastatin ketone 2 complex with fascin, the structures of migrastatin ketone 2 and migrastatin ether 4 have been re-evaluated by NMR and X-Ray crystallographic techniques. The results of these studies established the correctness of the previously reported structural assignment and confirm that the "small molecule" co-crystallized in complex with fascin is not the migrastatin ketone, which was provided for the infusion experiment, but rather its stereoisomer.
ABSTRACT
A significantly simpler analog of the natural product migrastatin, termed migrastatin ether (ME), has been prepared and evaluated. Both in vivo and in vitro studies indicate that ME exhibits a concentration-dependent inhibitory effect on migration of breast cancer cells.
Subject(s)
Antineoplastic Agents/pharmacology , Biological Products/chemistry , Breast Neoplasms/drug therapy , Cell Movement/drug effects , Ethers/pharmacology , Macrolides/pharmacology , Neoplasm Metastasis/drug therapy , Piperidones/pharmacology , Animals , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Antineoplastic Agents/therapeutic use , Breast Neoplasms/pathology , Drug Screening Assays, Antitumor , Ethers/chemical synthesis , Ethers/chemistry , Ethers/therapeutic use , Female , Humans , Macrolides/chemistry , Macrolides/therapeutic use , Mice , Molecular Conformation , Neoplasm Metastasis/pathology , Piperidones/chemistry , Piperidones/therapeutic use , StereoisomerismABSTRACT
A recent publication is a great example of the inherent potential of exploring the chemical space inspired by natural products. Expanding access to chemical space through organic synthesis allows the discovery of valuable new small-molecule mediators of biological activity.
Subject(s)
Antineoplastic Agents/pharmacology , Neoplasm Metastasis/drug therapy , Antineoplastic Agents/chemistry , Biological Products/chemistry , Biological Products/pharmacology , Humans , rho GTP-Binding Proteins/antagonists & inhibitorsABSTRACT
En 100 cadáveres del anfiteatro de anatomía macroscópica de la Facultad de Medicina de la Universidad de Cartagena, las secciones de morfología y neurologíadisecaron las arterias que irrigan el encéfalo. Se realiza una revisión de la anatomía y la clínica, con las consecuencias que pueden generarse ante la obstrucción de las arterias cerebrales, teniendo en cuenta que estas circunstancias son comunes en nuestra práctica clínica
