109789-39-1Relevant articles and documents
Design, synthesis and biological evaluation of estradiol-PEG-linked platinum(II) hybrid molecules: Comparative molecular modeling study of three distinct families of hybrids
Provencher-Mandeville, Josée,Debnath, Chhanda,Mandal, Sanat K.,Leblanc, Valérie,Parent, Sophie,Asselin, éric,Bérubé, Gervais
, p. 94 - 103 (2011)
The synthesis of a series of 17β-estradiol-platinum(II) hybrid molecules is reported. The hybrids are made of a PEG linking chain of various length and a 2-(2′-aminoethyl)pyridine ligand. They are prepared from estrone in only 5 chemical steps with an overall yield of 22%. The length of the PEG chain does not influence the solubility of the compounds as it remains relatively constant throughout the series. MTT assays showed that the derivative with the longest PEG chain showed the best activity against two human breast cancer cell lines (MCF-7 and MDA-MB-231). The novel PEG-hybrids are also compared in terms of activities with two other families of 17β-estradiol- platinum(II) hybrids that we reported in previous studies. Molecular modeling study performed on a representative member of each family of hybrids reveals distinct molecular interactions with the estrogen receptor α which further corroborates their notably contrasting cytocidal activities on breast cancer cell lines. This study also shows that lipophilicity and the orientation of the tether chain between the estrogenic portion and the platinum(II) core contribute markedly to the biological activity of the various families of hybrids. The most active hybrids are those possessing an alkyl tether chain at position 16β of the steroid nucleus. For example, derivative 3 (p = 6) is about 16 times more potent on MCF-7 breast cancer cells than the corresponding 16α-PEG-hybrids (2b) made in this study.
Synthesis of 17β-estradiol-platinum(II) hybrid molecules showing cytotoxic activity on breast cancer cell lines
Provencher-Mandeville, Josée,Desc?teaux, Caroline,Mandal, Sanat K.,Leblanc, Valérie,Asselin, éric,Bérubé, Gervais
, p. 2282 - 2287 (2008)
The synthesis of a series of 17β-estradiol-platinum(II) hybrid molecules is reported. The hybrids are made of a PEG linking chain of various length and a 2-(2′-aminoethyl)pyridine ligand. They are prepared from estrone in five chemical steps with an overall yield of 22%. The length of the PEG chain does not influence the solubility of the compounds as it remains relatively constant throughout the series. MTT assays showed that the derivative with the longest PEG chain showed the best activity against breast cancer cell lines (MCF-7 and MDA-MB-231). Molecular modeling study rationalized the results.
Conjugate of dezocine and polyethylene glycol
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Paragraph 0092; 0093; 0094, (2018/07/30)
The invention relates to the technical field of medicine, in particular to a conjugate of dezocine and polyethylene glycol as well as a pharmaceutical composition thereof. The conjugate of dezocine and polyethylene glycol, which is provided by the invention, has high pharmacokinetic property and high medicine absorbing degree, reduces the side effect of the medicine, and can realize smaller administration dosage and more administration modes such as oral administration in clinical practice; and compared with the dezocine, the conjugate provided by the invention has stronger analgesic effect and longer analgesic duration, can reduce the medicine use times and improve the compliance of a patient, and has the advantages in the aspects of effectiveness, safety, medicine resistance and the likeof the medicine.
Polyacrylamide pseudo crown ethers via hydrogen bond-assisted cyclopolymerization
Kimura, Yoshihiko,Miyabara, Yuichiro,Terashima, Takaya,Sawamoto, Mitsuo
, p. 3294 - 3302 (2016/09/09)
Polyacrylamide pseudo crown ethers with large in-chain rings (15–24 membered) were synthesized by hydrogen bond-mediated cyclopolymerization of bisacrylamides comprising poly(ethylene oxide) spacers (PEGnDAAm, ethylene oxide units: n = 3–6). The monomers undergo the intramolecular hydrogen bonding of the bisacrylamide units in halogenated solvents to dynamically place the two olefins adjacently. As a result, the bisacrylamides homogeneously allowed controlled radical cyclopolymerization without any macroscopic gelation in 1,2-dichloroethane, even at relatively high concentration of monomers (200 mM), to directly provide precision cyclopolyacrylamides and the related copolymers with high cyclization efficiency (84–98%). Owing to the in-chain ring pendants, a cyclopolyacrylamide had glass transition temperature higher than a corresponding polyacrylamide with linear pendants.
