Gunda I. Georg, et al, “Novel Biologically Active Taxol Analogues: Baccatin III 13-(N-(p-Chlorobenzoyl)-(2′R,3′S)-3′-phenylisoserinate) and Baccatin III 13-(N-benzoyl-(2′R,3′S)-3′-(p-chlorophenyl)isoserinate),” Bioorganic and Medicinal Chemistry Letters, 2(4), pp. 295-298, 1992. |
Gunda I. Georg, et al, “Semisynthesis and Biological Activity of Taxol Analogues: Baccatin III 13-(N-benzoyl-(2′R,3′S)-3′-(p-tolyl)isoserinate), Baccatin III 13-(N-p-toluoyl)-(2′R,3′S)-3′-(phenylisoserinate), Baccatin III 13-(N-benzoly-(2′R,3′S)-3′-(p-trifluoromethylphenyl)isoserinate), and Baccatin III 13-(N-(p-trifluoromethylbenzoyl)-(2′R,3′S)-3′-phenylisoserinate),” Bioorganic and Medicinal Chemistry Letters, 2(12), pp. 1751-1754, 1992. |
Gunda I. Georg, et al, “Synthesis of Biologically Active Taxol Analogues with Modified Phenylisoserine Side Chains,” Journal of Medicinal Chemistry, 35, pp. 4230-4237, 1992. |
F. Gueritte-Voegelein, et al, “Relationships Between the Structure of Taxol Analogues and Their Antimitotic Activity,” Journal of Medicinal Chemistry, 34, pp. 992-998, 1991. |
D.G.I. Kingston, et al, “The Chemistry of Taxol, A Clinically Useful Anticancer Agent,” Journal of Natural Products, 53(1), pp. 1-12, 1990. |
Larry L. Klein, “Synthesis of 9-Dihydrotaxol: A Novel Bioactive Taxane,” Tetrahedron Letters, 34(13), pp. 2047-2050, 1993. |
Julio C. Medina, et al, “A Mild Method for the Conversion of Alcohols to Methylthiomethyl Ethers,”Tetrahedron Letters, 29(31), pp. 3773-3776, 1988. |
K. C. Nicolaou, et al, “Design, Synthesis and Biological Activity of Protaxols,” Nature, 364, pp. 464-466, Jul. 29, 1993. |
Iwao Ojima, et al, “New and Efficient Approaches to the Semisynthesis of Taxol and Its C-13 Side Chain Analogs by Means of β-Lactam Synthon Method,” Tetrahedron, 48(34), pp. 6985-7012, 1992. |
Iwao Ojima, et al, “Efficient and Practical Asymmetric Synthesis of the Taxol C-13 Side Chain, N-Benzoyl-(2R,3S)-3-phenylisoserine, and Its Analogues Via Chiral 3-Hydroxy-4-Aryl-β-Lactams Through Chiral Ester Enolate-Imine Cyclocondensation,” Journal of Organic Chemistry, 56, pp. 1681-1683, 1991. |
Iwao Ojima, et al, “New and Efficient Routes to Norstatine and Its Analogs with High Enantiomeric Purity by β-Lactam Synthon Method,” Tetrahedron Letters, 33(39), pp. 5737-5740, 1992. |
Muhammad Safadi, et al, “Phosphoryloxymethyl Cabamates and Carbonates—Novel Water-Soluble Prodrugs for Amines and Hindered Alcohols,” Pharmaceutical Research, 10(9), pp. 1350-1355, 1993. |
G.H. Veeneman, et al, “An Efficient Approach to the Synthesis of Thymidine Derivatives Containing Phosphate-Isosteric Methylene Acetal Linkages,” Tetrahedron, 47(8), pp. 1547-1562, 1991. |
Dolatrai M. Vyas, et al, “Synthesis and Antitumor Evaluations of Water Soluble Taxol Phosphates,”Bioorganic and Medicinal Chemistry Letters, 3(6), pp. 1357-1360, 1993. |
N. Gerber, et al, “Safety, Tolerance and Pharmacokinetics of Intravenous Doses of the Phosphate Ester of 3-Hydroxymethyl-5,5-Diphenylhydantoin: A New Prodrug of Phenytoin,” J. Clin. Pharmacol., 28, pp. 1023-1032, 1988. |
Albert S. Kearney and Valentino J. Stella, “Hydrolysis of Pharmaceutically Relevant Phosphate Monoester Monoanions: Correlation to an Established Structure—Relativity Relationship,” Journal of Pharmaceutical Sciences, 82(1), pp. 69-72, Jan., 1993. |
Theodora W. Greene and Peter G.M. Wuts, “Productive Groups in Organic Synthesis,” Second Edition, pp. 10-12, 14, and 413, John Wiley & Sons, Inc., USA, 1991. |
J.H. Jones, et al, “t-Butyl Chloromethyl Ether,” Syn. Comm., 16(13), pp. 1607-1610, 1986. |
I.R. Jack, “Unambiguous Synthesis of 2,4-Diphenyl-3,7-Dioxabicyclo[3.3.0]Octane,” Ind. J. Chem. 28B, pp. 454-456, 1989. |
Y.H. Park, et al, “Structure-Activity Relationship (SAR) Study on Taxol and Taxotere Analogs Derived from New Baccatins,” 205th American Chemical Society National Meeting in Colorado (Med. Chem. Division, Abstract No. 28), 1993. |
I. Ojima, et al, “A Highly Efficient Route to Taxotere by the β-Lactam Synthon Method,” Tetrahedron Letters, 34(26), pp. 4149-4152, 1993. |
R.A. Holton, et al, “A Novel Asymmetric Synthesis of CIS-3-Hydroxy-4-Aryl Azetidin-2-Ones,” Bioorganic and Medicinal Chemistry Letters, 3(11), pp. 2475-2478, 1993. |
I. Ojima, et al, “N-Acyl-3-Hydroxy-β-Lactams as Key Intermediates for Taxotere and its Analogs,” Boorganic and Medicinal Chemistry Letters, 3(11), pp. 2479-2482, 1993. |
G.I. Georg, et al, “An Efficient Semisynthesis of Taxol from (3R,4S)-N-Benzoyl-3[(t-butyldimethylsilyl)oxy]-4-phenyl-2-azetidinone and 7-(triethylsilyl)baccatin III,” Bioorganic and Medicinal Chemistry Letters, 3(11), pp. 2467-2470, 1993. |
R. Brieva, et al, “Chemoenzymatic Synthesis of the C-13 Side Chain of Taxol: Optically-Active 3-Hydroxy-4-Phenyl β-Lactam Derivatives,” J. Org. Chem., 58, pp. 1068-1075, 1993. |
C. Palomo, et al, “Highly Stereoselective Synthesis of α-Hydroxy β-Amino Acids Through β-Lactams: Application to the Synthesis of the Taxol and Bestatin Side Chains and Related Systems,” Tetrahedron Letters, 31(44), pp. 6429-6432, 1990. |
D.A. Scudiero, “Evaluation of Soluble Tetrazolium/Formazan Assay for Cell Growth and Drug Sensitivity in Culture Using Human and Other Tumor Cell Lines,” Cancer Res., 48, pp. 4827-4833, 1988. |
W. Rose, “Evaluation of Madison 109 Lung Carcinoma as a Model for Screening Antitumor Drugs,” Cancer Treatment Reports, 65, No. 3-4, pp. 299-312, 1981. |
W.C. Rose and G.A. Balser, “In Vivo Model Development of Cisplatin-Resistant and -Sensitive A2780 Human Ovarian Carcinomas,” In-Vivo, 4, pp. 391-396, 1990. |
W.C. Rose and G.A.Balser, “An In Vivo Human Tumor Xenograft Model of Etoposide Resistance,” In-Vivo, 3, pp. 249-254, 1989. |
J.-N. Denis, et al, “A Highly Efficient, Practical Approach to Natural Taxol,” J. Am. Chem. Soc., 110, pp. 5917-5919, 1988. |
Greene et al, “Protecting groups in Organic Chemistry”, 2nd ed, pp 10-12, 413, 1991. |