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Three new cationic gemini surfactants with ester spacer type 2-2'-(ethane-1,2-diyl bis(oxy)) bis(N-(2-alkanamidoethyl)-N,N-dimethyl-2-oxoethan-1-aminium)) dichloride) (CGSES12, CGSES14 and CGSES16), based on ,-dimethyl fatty amido ethylamine, were produced. These gemini quaternary ammonium salts were synthesized using a three-step reaction method, starting from th/e condensation of the fatty acid chloride (RCOCl) of various hydrophobic chain lengths (R, CH, CH, CH) with ,-dimethyl ethylene diamine, followed by the quaternization of the tertiary amino group formed with the spacer of the ester group formed in the second step. The chemical configuration of the surfactants was established by FT-IR, HNMR, CNMR and Mass spectroscopies.

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Article Synopsis
  • The study investigated the effectiveness of the telomerase inhibitor imetelstat in treating osteosarcoma, a type of bone cancer, using pre-clinical models.
  • Results showed that imetelstat alone decreased telomerase activity, caused telomere shortening, and inhibited growth in osteosarcoma cell lines, but didn't fully stop cell growth in bulk cultures.
  • The combination of imetelstat and the HSP90 inhibitor alvespimycin led to increased DNA damage and complete growth arrest in cell cultures, and also significantly reduced tumor growth in xenograft models, suggesting that dual targeting is a promising therapeutic strategy.
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We describe here the synthesis and characterization of new sulfonated and carboxylated-containing N-donor ligands [Na(4)(edts)]·4H(2)O (2), [Na(2)(dmeddp)]·2H(2)O (3) and [Na(4)(edtp)]·H(2)O (4) (edts = ethylene-diamine- N,N,N',N'-tetraethylenesulfonate ion; dmeddp = dimethyl-ethylene-diamine-N,N,N',N'-tetra-3-propionate ion; edtp = ethylene-diamine-N,N,N',N'-tetra-3-propionate ion) and their corresponding metal (Ni, Co, Cu and Zn) complexes. Mainly, UV-Vis and a computer aided analysis of the EPR spectra provided information on the geometry and structure of the complexes in solution. Some of the metal complexes inhibit HIV replication when treating both pre- and post-infected PBMC cells, and hustle the inhibitory effect compared to the metal salts alone.

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17-Allyamino-17-demethoxygeldanamycin and 17-NN-dimethyl ethylene diamine-geldanamycin have cytotoxic activity against multiple gynecologic cancer cell types.

Gynecol Oncol

February 2005

Department of Obstetrics and Gynecology, University of Michigan Medical Center, Med. Sci. II, 1500 E. Medical Center Drive, Ann Arbor, MI 48109-0618, USA.

Objective: HSP90 is a cellular chaperone that is overexpressed in many cancers. HSP90 assists in proper folding of a variety of clients, many of which are oncoproteins. HSP90 has been shown to be elevated in endometrial, ovarian, and breast cancer.

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