77406-93-0Relevant articles and documents
Polymer conjugates of the highly potent cytostatic drug 2-pyrrolinodoxorubicin
Studenovsky,Ulbrich,Ibrahimova,Rihova
, p. 156 - 163 (2011)
This paper describes the synthesis and biological evaluation of a conjugate of the highly cytotoxic drug 2-pyrrolinodoxorubicin (p-DOX) with an N-(2-hydroxypropyl)methacrylamide copolymer (PHPMA) as a water-soluble biocompatible polymer carrier, utilizing the advantageous concept of polymer-drug conjugates. The conjugate of p-DOX with HPMA copolymer (PHPMA/p-DOX) was prepared by reacting the PHPMA/DOX conjugate, where the DOX was bound via a hydrazone bond, with 4-iodobutyraldehyde. The hydrazone bond between the polymer and drug is susceptible to pH-controlled hydrolysis, enabling prolonged stability in circulation and fast p-DOX release under conditions mimicking the intracellular environment. The in vitro cytostatic activity of free p-DOX was in accordance with literature, whereas its PHPMA conjugate exhibited a 1.3- to 5-fold lower cytotoxicity, depending on the cancer cell line, when compared to the free p-DOX. This is in qualitative agreement with the data obtained for DOX and its HPMA copolymer conjugates. On mice bearing T-cell EL4 lymphoma, no tumor suppression was observed from the free p-DOX at a subtoxic dose of 0.1 mg/kg, whereas the PHPMA/p-DOX conjugate significantly inhibited the initial tumor growth at approximately equitoxic doses of 0.4 and 0.8 mg p-DOX eq/kg. However, moderately elevated doses of the p-DOX equivalent in the conjugate caused toxic effects, making accurate dosage setting essential.
Oxidative opening of cycloalkanols: An efficient entry to ω-iodocarbonyl compounds
Barluenga, Jose,Gonzalez-Bobes, Francisco,Ananthoju, Sreenivasa R.,Garca-Martn, Miguel A.,Gonzalez, Jose M.
, p. 3389 - 3392 (2007/10/03)
Simply mix and switch on the light: This is all that is required to obtain ωfunctionalized aldehydes and ketones from readily available cyclic alcohols and IPy2BF4. The unusual oxidation process is outlined in Equation (1). R1/
Controlling the Outcome of a Carbocation-initiated Cyclisation
Chow, Hak-Fun,Fleming, Ian
, p. 1815 - 1819 (2007/10/02)
The Z- and E-vinylsilanes, 6,6-dimethoxy-2-methyl-1-trimethylsilylhex-1-ene (6), gave only 3-methoxy-1-methylcyclohexene (7) on treatment with zinc bromide, and the allylsilane, 6,6-dimethoxy-2-methyl-3-trimethylsilylhex-1-ene (8), gave only 5-methoxy-1-methylcyclohexene (9) on treatment with tin(IV) chloride.Taken together with an earlier result, these results show that the silyl group completely controls the outcome of this carbocationic cyclisation.The syntheses of the two starting materials, (6) and (8), illustrate the usefulness of the silyl-cuprate reagent in the costruction of specific vinyl- and allyl-silanes.