Synthesis and Antitumor Activity of O- and N-Propylamino-Derivatives of Betulin

Chemistry of Natural Compounds - O- and N-propylamino-derivatives of betulin and betulonic acid oxime and methyl ester were synthesized. Their antitumor activity against a panel of 60 human cancer...     

Synthesis and Pharmacological Activity of 20-Keto-29-norlupane Derivatives

New 20-oxo- and hydroxyimino-derivatives of betulin that exhibit immunotropic and antiviral activities were synthesized. __________ Translated from Khimiya Prirodnykh Soedinenii, No. 6, pp. 582–584, November–December, 2005.     

Effective synthesis of methyl 3β-amino-3-deoxybetulinate

A practical method for preparing methyl 3β-amino-3-dexoybetulinate that is based on column chromatographic separation of 3α- and 3β-t-butoxycarbonates and subsequent removal of the protecting group using formic acid is proposed. The structure of methyl 3β-N-(t-butoxycarbonyl)-3-deoxybetulinate was established by an x-ray structure analysis. Translated from Khimiya Prirodnykh Soedinenii, No. 5, pp. 488–490, September-October, 2008.     

Reactions of 2-pyrimidinyl phosphites with proton-containing nucleophilic reagents

Conclusions The reaction of 4,6-dimethyl-2-pyrimidinyl phosphites with proton-containing nucieophilic reagents is due to the anhydride nature of the C_pry-O-P bond and proceeds with the formation of 4,6-dimethyl-1,2-dihydro-2-pyrimidone and the corresponding P(III) derivatives.Translated from Izvestiya Akademii Nauk SSSR, Seriya Khimicheskaya, No. 1, pp. 159–162, January, 1986.     

Synthesis of new betulonic and oleanonic acid amides

Amides of betulonic and oleanonic acids with diethylenetriamine, triethylenetetramine, and spermidine were synthesized. Antitumor activity in vitro was not found for the conjugate of betulonic acid with diethylenetriamine.     

Synthesis and physicochemical properties of [{Cd(?-C6H11NO)5}2Cr(NCS)6][Cd(?-C6H11NO)4Cr(NCS)6]

A new complex [{Cd(?-Cpl)₅}₂Cr(NCS)₆][Cd(?-Cpl)₄Cr(NCS)₆] was synthesized, and its crystal structure was solved. The complex was studied by chemical analysis and IR spectroscopy.     

Synthesis,Anti-Influenza H1N1 and Anti-Dengue Activity of A-Ring Modified Oleanonic Acid Polyamine Derivatives

A series of sixteen A-ring modified (2,3-indolo-, 2-benzylidene) oleanonic acid derivatives, holding some cyclic amines, linear polyamines and benzylaminocarboxamides at C28, has been synthesized and screened for antiviral activity against influenza A/PuertoRico/8/34 (H1N1) and Dengue virus serotypes of DENV-1, -2, -3, -4. It was found that 28-homopiperazine 2 and 3-N-phthalyl 22 amides of oleanonic acid demonstrated high potency with selectivity index SI 27 (IC₅₀ 21 μM) and 42 (IC₅₀ 12 μM). Oleanonic acid aminoethylpiperazine amide 6 and C-azepano-erythrodiol 23 appeared to be the most effective compounds against DENV-1 (IC_50′s 67 and 107 μM) and -2 (IC_50′s 86 and 68 μM correspondingly) serotypes.