Antileukaemic activity

Acetamides of type (83) derived from various /V-heterocycles have been prepared and investigated for antileukaemic activity in the German Democratic Republic. Within this series, the pyridazine derivative (84) was found to be the only active compound inhibiting the growth of L-1210 mouse cells in vitro (IDS0 10 4 mol/I) [297],... 

Quassinoids —The antileukaemic activity of some quassinoids has revived interest in this group. Three new biologically active compounds have been isolated. Quassimarin (118) occurs in Quassia amara with the inactive simalikalactone D (129) 86 Bruceoside A, from Brucea javanica, is the glucoside (120). The third... 

Some positional isomers of coralyne have been synthesized and examined for antileukaemic activity,82 and the distribution of salts of coralyne after they have been administered to rodents has been studied.83 Dehydrogenation of canadine to berberrubine (59) can be accomplished in ethylene glycol and hydrochloric acid with palladium or with tris(triphenylphosphinyl)rhodium chloride, the reaction proceeding faster at low temperatures with the latter catalyst.84 Derivatives of 13-methylberberrubine and its analogues have been synthesized, so that they might be screened to find their potential as antitumour agents.85... 

Kupchan, S.M., Komoda, Y., Branfman, A.R., Dailey, R.G., Zimmerly, V.A. Novel maytansioids. Structural interrelations and requirements for antileukaemic activity. 

Colorimetric and volumetric assays and radioimmunoassay of colchicine have been described. Various thiocolchicines have been prepared and tested for antileukaemic activity. Haematological effects have been noted for N-... 

Various workers have attempted the chemical 77-80 or microbiological81 modification of quassinoids in the search for compounds with potent antileukaemic activity. 

Pyrroloazepines are of interest partly because of the antileukaemic activity of some compounds that contain the l//-pyrrolo[2,l-6][3]benzazepine moiety. The new 5H-pyrrolo[l,2-6][2]benzazepine system has been synthesized via the base-induced cyclization of the key intermediate (39), followed by hydrolysis and decarboxylation to give the parent nucleus. 

The antileukaemic activity of colchicine derivatives"" and their effects on RNA synthesis,on intestinal disaccharidase activity," " and on the secretion of parathyroid hormone" have been studied. 

A range of imidazo-fused C-nucleosides with bridgehead nitrogen of the general type (44,X,Y=CH or N) have been prepared, and the somewhat similar pyrazolotriazine (45) shows good antileukaemic activity the corresponding 4-thiocompound has also been reported. Cycloaddition of maleimlde to 2-... 

The discovery that arabino-cytxddae shows antileukaemic activity has prompted the synthesis of 5-(j8-D-arabinofuranosyl)-isocytosine (71) and some related C-nucleosides. The ara mo-nucleoside was synthesized from the corresponding antileukaemic 5-(j3-D-ribofuranosyl)-isocytosine by epimeriza-tion at C-2 via a 2, 4-anhydro-arabinosyl nucleoside intermediate. The a-anomer of (71) was also obtained. None of the new products showed any antileukaemic activity. ... 

Chemical modification of vinblastine has shown that antileukaemic activity against P-1534 is destroyed by removal of the acetoxy group, acetylation of the tertiary hydroxyls, or reduction of the methoxycarbonyl groups... 

The cyclopropane 208 could be prepared in high diastereomeric excess by treatment of the cis-alkene (derived from L-gulonolactone) with Et2Zn/CH2l2-Subsequent manipulation, including a Curtius reaction, then gave the L-nucleo-side analogues 209. There has also been a full account of work first reported last year (Vol.28, p.298) in which similar chemistry is used to prepare structures such as 209, but in the enantiomeric series. The wew-cyclopropane 210 has also been described, as has the racemic spirocompound 211, which has antiviral and antileukaemic activity. "... 

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