- Stereoelectronic factors influencing the biological activity and DNA interaction of synthetic antitumor agents modeled on CC-1065
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The synthesis, physicochemical properties, and biological activities of a series of novel spiro cyclopropyl compounds, modeled on the potent antitumor antibiotic CC-1065 (1), are described. Many of these synthetic analogues are significantly more effectiv
- Warpehoski,Gebhard,Kelly,Krueger,Li,McGovren,Prairie,Wicnienski,Wierenga
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p. 590 - 603
(2007/10/02)
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- Total Synthesis of U-71,184, A Potent New Antitumor Agent Modeled on CC-1065
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The synthesis of U-71,184 (2), a highly potent analog of the novel antitumor antibiotic CC-1065, is described, the penultimate step of which involves the unmasking of a p-hydroxy phenethyl mesylate, which undergoes facile intramolecular elimination to aff
- Warpehoski, M.A.
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p. 4103 - 4106
(2007/10/02)
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- Preparation and Stability of 1,4-Oxathian-2-ones
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Several methods of preparation of various substituted 1,4-oxathian-2-ones are described, including the acid-catalyzed ring closure of δ-hydroxy acids, prepared via α-halo ketones or α-halo acids, and the base-catalyzed ring closure of β-haloethyl thioglycolate. 1,4-Oxathian-2-one is completely hydrolyzed in D2O to the hydroxy acid at a rate comparable to the hydrolysis of δ-valerolactone.The rate of the lactonization is estimated to be ca. 100 times smaller in oxathianone than in valerolactone.
- Koskimies, Jorma K.
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p. 101 - 108
(2007/10/02)
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