- Synthesis, physicochemical, and biological activities of novel N-acyl tyrosine monomeric and Gemini surfactants in single and SDS/CTAB–mixed micellar system
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A series of single-chained N-acyl tyrosine surfactants with varying chain lengths (C10-C18) and degree of unsaturation, as well as an N-acyl Gemini tyrosine surfactant with chain length C12, were synthesized, and the struc
- Joondan, Nausheen,Jhaumeer-Laulloo, Sabina,Caumul, Prakashanand,Akerman, Matthew
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- STEAROYL AMINO ACID SALT AND PREPARATION METHOD AND APPLICATION THEREOF
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A stearoyl amino acid salt having a structural formula of the general formula (I), wherein R1 is H or an aromatic base capable of being substituted by one or more substituents, or a C1-4 straight chain or an alkyl with a branched chain, the substituent being an alcoholic hydroxyl group or a phenolic hydroxyl group; and R2 is a C11-25 saturated or unsaturated aliphatic group. Also provided are methods of preparing the stearoyl amino acid salt, and methods of using the stearoyl amino acid salt. Compared to a prototype drug stearoyl amino acid, the stearoyl amino acid salt described herein has excellent physicochemical properties, good stability, high relative bioavailability, a strong drug effect and a high safety factor. It is thus expected to become a candidate for clinical treatment of neurodegenerative diseases and acute brain injury, and a clinical drug for weight loss, thus having broad application prospects.
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- Synthesis and evaluation of anti-tumor activities of N4 fatty acyl amino acid derivatives of 1-β-arabinofuranosylcytosine
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1-β-d-Arabinofuranosylcytosine (Ara-C, Cytarabine) is one of the drugs used for acute nonlymphocytic leukemia (ANLL). However, the bioavailability of Ara-C is relatively low due to its low lipophilicity. In order to improve the lipophilicity and bioavailability of Ara-C, a series of N4 derivatives of Ara-C, i.e., (fatty acid)-(amino acid)-Ara-C analogues, were prepared. The 15 derivatives synthesized were characterized by their melting points, optical rotations and partition coefficients. It was found that the Ara-C derivatives synthesized in this study were more lipophilic than Ara-C as determined by their partition coefficients. Their in vitro cytotoxicity and in vivo anti-tumor activity were determined and compared with that of Ara-C. It was found that the derivatives were more active than Ara-C in Hela cells, but not in HL-60 cells. The in vivo results showed that some of the derivatives were more effective than Ara-C in mice bearing S180 tumor while others showed a decreased activity in comparison with Ara-C.
- Liu, Boyang,Cui, Chunying,Duan, Wei,Zhao, Ming,Peng, Shiqi,Wang, Lili,Liu, Hu,Cui, Guohui
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scheme or table
p. 3596 - 3600
(2009/12/04)
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- Synthesis and biological evaluation of phosphonate derivatives as autotaxin (ATX) inhibitors
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Autotaxin (ATX) is an autocrine motility factor that promotes cancer cell invasion, cell migration, and angiogenesis. ATX, originally discovered as a nucleotide phosphodiesterase, is known now to be responsible for the lysophospholipid-preferring phosphol
- Cui, Peng,Tomsig, Jose L.,McCalmont, William F.,Lee, Sangderk,Becker, Christopher J.,Lynch, Kevin R.,Macdonald, Timothy L.
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p. 1634 - 1640
(2007/10/03)
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