SCIENTIFIC ABSTRACT VARGHA, L. - VARGIN, V.V.
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CIA-RDP86-00513R001858620007-4
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S
Document Page Count:
100
Document Creation Date:
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Document Release Date:
August 9, 2001
Sequence Number:
7
Case Number:
Publication Date:
December 31, 1967
Content Type:
SCIENTIFIC ABSTRACT
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Vi'MIIA L. C Ca'KAY, Gy.
Stereospecific conversions in the furyl-2-ketoxime series. p.143
ACrA,CHIMICA. Buda0est, Hungary, Vol. 19, no.2/3. 1959
Monthly List of East European Accessions (F~--), LC. Vol. 8, No. 9, September 1959
Uncl.
O~a~ ~W
Synthesis of new sugar derivatives of potential anitiumor activity. III. On
2-halogeno-ethylamino- and othyleneimino derivatives of sugar alcohols. p.295
ACTA CHIMICA. Budapest., Hungary. Vol. 19,, no.2/3j. 1959
Monthly List of East European Accessions (EELI), LC. Vol. 8, No. 9, September 1959
Hal.
VARGHA,, L FEHER, 0 LENDVAI., S.
Synthesis of now sugar derivatives of potential antitumor activity. IV, On
2-dichloro-dyethilamino derivatives of monosaccharides. P-307
ACTA CHIMIGA. Badapest, Hungary. Vol. 19., no. 2/3j, 1959
Monthly List of Best European Accessions (EEAI)., LC. Vol. 8., No. 9j. September 1959
Uncl.
TOLDY, Lajos; VARGRA, Laszloz TOTH, Istvan; BCIRSY, Jozaef
fr1cmthazins investigations. Pt. 1. Magy kem folyoir 65 no.1-4-1
ja 159 a,
10 Gyogyszeripari Kutato Intezeto
TOLDYO Lajos, a kemiai tudomanyok kandidatusa (Budapest); VARGHA, Laszlo,
(Budapest)
Benzal derivatives of T Iditol. Kem tud kozl MTA 13 no.1:51-58 160.
(EEAI 10:2)
1. Oyogyszeripari Kutato Intezet, Budapest. 2. Levelezo tag
Magyar Tudmaroroa Akademia (for Vargha)
(Benzal groups) (Iditol)
VARGIIA, Laszlo, dr., Kosouth-dijas (Budapest)
Achievements and cares; Academician and Kosouth-Prize wInner Dr. Laszlo
Vargha on the present and perspectives of our pharmaceutical research.
Ujit lap 13 no.23:8 D 161.
1. Igazgato, Oyogyszeripari Kutato Intezet, Budapest.
URGHA, L.; TOLDY, L.; iLl0i, 0-,,; HOITIVATI!, T,- KASZT174EEMER, El. KUSZl-WV',
IJVJI-L, Sarolta
New sug&r derivatives vith cytostuatic effectiveness, Acta
hung. 19 no.1-4:305-312 `61,
1. Forschunginstitut fur die phar-..,azoutische industrial Budapest,
(CARBOHMUTES p1mrma-loey)
(ANTINEOPUSTIC AGENTS phax mac.ology)
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The somisstildrs 91 formed
*11h dicaftiottille fields. LASS16 Vvillilm. JbICISIP 111-4
Wj 1.,14 1.
NII, ll~Alul (0hvA 11k-fit, r,61 -00
sills-frd, washril .411 Slid likuhtl tbthv Iliker with *.,.it X
1111140
NsOll. Thv pptd. Nis ult wakk dm~klvvd lit dil. lICI and .
recryqtd. The pure product ",c;M~tcd ofctkI(wk-"ncedIc,%, 600
lit. of p.jIC)iCCI)N 11C.11,"A NN 111. 1 di-
noto
.4veil in hol watcr, aithyd. Na,%:tlI -loil 1101CCII'COO
liddell. Owli t"Ar.1 MI A with 110 1 lie pf,iihi, 1 0
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Wd'I P-M),CC11.0 III I*,*V. I Willi
is
not
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CIIXON IIC,li..-'A),.N lit 111) its. 212".
goo
heated Willi Milipir Ovid &&",I thr 1-Ited llii%t. wil-di-lik"I o*
in 1401; N.'CIN. lh~ 114,1 4t..- s
of ill I't
I Willi .611hy.1, 1,110141%. ..%1 It,". I.
'
m 14.4. .1
N11C.Ii.S4 4
Ihrrapicutic viltvi of the dvrivs. agaiu,t kkirvintwoct-ti,; sit.
moo
Irclitills. H secturd it) have (lit- -Irmlitc,t dointv,,tinst
dV PinAtv
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0411 a Some now derivatives at pbenythydraxlno~ AA,-Al 00
Varghn (Chem. Factory Richter Budapw.
004 Kuw6inthd AfaaW 14, 441-4(194!1).-
The oblect was tm Prep. derivs. o( PhNIINIft hAving vulu.
able pharm". proliertke without a toxicity higher than .00
0 that of d1hydrotypyrandlinne. I-Mityl-l-Irnsulil-1-
(1). prwpd. frLxn 1140,11INHAv, suqwn.fird
j lit anhyd. C,1-14 and rrduxtd 2 firs. with 11M. cvAe1c%% ne"I -
Irs, ms. 154'. An sk. suniension of I with bfc*SO, and No
0: 4 lit with Orong cooling led to calmicas needles of I-phenyl:
I-bem-vi-2-wvtyi-24nrthylhydraiine(II).m.114'. Simi- coo
far tmalment of I with Et#SO. led to rokirlims amik-s o(
I-l,heLnvf-l-beuvyyt-2-wvtyl-2-cth)ihyltt"ric fill). in. -00
0911 IZ"*. Similarly, PhVAcVIIAc gave I -pbettyl-
yl -2-awthythydriazine (IV). colorlen liquid. b. 175-9*. 11
wwq Invii. in water, and showed strong, hosting a .Pr !coo
an nz
Is and apralCiijk tferls In sewre hirmayiris. M W"
in water and teentied to be toxic but showed no rtflabk
phamarNopic effecti. IV, water-sol., was at Ineffective
and ntint(We as dibydrrixypyriamidont. Istivin Finkly
:1 i woo
4 or
.1 NITALLUKKAL L179RATLIL CLAISWKATICO, 9 1 zz- e 0 0
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Tho bialatical 440111CAM4 d Offitil 01 VWkOk
"Woo of DIM011C add. co. Irknovici and L. Vorgha
(fintly NMI?" Univ. sel-VA. flu"Kary). Z' Obvid.
CASM. U1. to def. the functiott
of pinielke. airid (1) In the growth e4 certain bacteria by
eml4aying sulfanic acid analogs clf 1 as competitive in-
hillitors are dt-uTiLed. 115-Pentanedijulfamic acid, 1,5-
ptnflatl OM~Altllllnilfe, 41-1111 OC41WOle arid (11). and d-
S a ase and (111) were uspd and foutut to be in-
ive as tibibilors. The synthesis of 11 and M Is de-
"bed: 9 g. .-bramoraproic acid (IV) refluxed with A g.
KIIS and R) cc. H-0 2 hri., colAing. adda. of IFISO,, and
eurt. with ethet give Rnel, .-marraploralwoic 4rU (Y). N3
IW~V- SaIn. with CI (4 7 It. V in 71) cc, glacial AcOll
at 15'. 4tanding 3 hr,%.. removal 4 the ALMI in vatua.
and cMtn. front petr. ether give% F07c o(eklorojulfila)1).
IlO 2 hill.
VI rrfluxed with I
14
orid (VI), in, 90. ich vt converted tot
ed gives 11 as an (A wh he di -N&
salt. inull. in E1011. VI added slowly to ice-COM coned,
-NI1,011, dr3ing. UA er"In. Irnm arvtone-Clich gives
K5c' , Ill. m. lo:,*. Nn salt of ID, Sparingly got. in 967.
HIM. tims not lit. :))5*. C3 sjtn. of V or water sus-
I L a NTALLOUr-a UMIIATW
I'le4`101 nIPOIF VgiJr!!r27t15O1" off tShCcllPrfordlttlc,)t,.ratn),dffrie,cr"to. from
, rn. M31.
Iquirroll. aulug. d I
V and C,9(NII,),, heated 3 hn. in
AmOll at I cooling. ths(n. of the "~qvrrtt. W)rn.
'At tile r-illue in Ill(). n-t'Aic"ti- with Vololl. Voln.
(d the filtered pill. in (fit. IM. drying. alul crysta. from
FtOlf-ether give 65'r *-1A1*4nn`eUACdprOiC 4fid.MCI. M.
1(01'. Addn. Of V1 to'cw4tA 1q. Mr,'S'11. widn. a( IJCJ.
clint-u., still rrcrysin. (folii triurne give o4dintr4hyl.
tulfamyhcuppok uirl, m. OV. 1.5-Pentancifisulfonyl
chlorick. tn-ated with %Iet%lf a- above gives
leframtthyt-1,5-pexknrdis3ilfowmide, m. Ful". The bac-
leriol. ezptq. are dr%cribr,1 Karl P. Urbach
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1, 711,
I %%1UMSUet blolorjcally Astive new Chfonlane derivittivos.
*1~4rfil, flIllartil, Rm,:irch L!LJ., fill,
Srs. Jbing, 3, :.'23-909,531*.;
(1) oblaint-d i's
Yijd fly Ire4ling 4A) X, N.1 t"'o,~fIrr Trish 11 F:. 2"71.1'"
(11). Uo Fill, al", 17.1011. lifid 1; 1 K.
(ftolu alk: ). I ( I S 10 W "0 ml,
al)4. FtOlt treatcd with 2 nil. coned. IICI mid the priAtict
puril'ied in ractic gi% es 4 g.-of it labile exanhwi fall (111), ill.
MA43W; 1110 g.) Ticated 15 -nin. fit IN) nil. dio\;me givr%
3.5 9. (IV). ni. 1:!!I-',In*;
Oxhite, its, 167-8.5'. :.
(V), obtained in 26 g. 3 ield by wming I'D Ct g - 11 atid 1:1.8
g, (COljFt)s with OA) g. Na fit 30) nil. ab~. FtOl I wid tri.
turating the Na salt with 10% IIC'Ac, m, 83-7* (from If.-O).
acid (VI) E'l-rilrr (VII),
obtained fit 90% yield by licating 19.0 g, V fit 150 tal.
aciat 11OAc va . colicd. IICI, m. 173-A' (from nic.).
(ill 8 nil
V1, obtained fit 70% yield by heating 27.8 g. VN 0 hn. ill
160 mi. glacial IIOAc with 200 nil. 4N llrSO#, m. 230-1*
(from HOAc), forms no oxime. Bit ester of V1 obtained In
60% yield from 2.6 g. VI, 250 ml. BuOH, and 20 g. coned.
112$O# refluxed 6 hr3., dild. with 110H, and neutralized
with NaHCOl, m. 05-6' (from 6070 MeOll), forms no
-oxitne. 6,7-Diriteth,7xychrot)totte-2-carboxylic acid (C.A. 44,
7317a) (25 9.), in 400 ml. BuOH and 140 g. coned. 11,SO4
refluxed 8 firs., dild. with H011, and neutralized with
MILO% gives t8.5 g. Bu ester, tn. 131-2.5' (from 75,70
iii1c.). The presence of the -AfeO groups enhances the
hnarmacol. activity of the chromone derivs. similar to IV
ut has little effect if a carlwityl group Is already preseni
g
the position of the AfcO groups seems to be unlinilortant.
R. W. Rqt:lqrA-Jx-l
- . . 1, -. ~z ~ ,4, -A
- . ~~;
- ~ '~ k, -.
. ,I : . .,; ,
-"--.-.VARGILk,-Ka1man-__
Data on the investigation of the white active filling materials.
Magy kem lap 17 no.5:212-216 My 162.
1. Bca-ipari Kutato Intezet.
VIA-r5lia-mue -awl El--
yo
a mn.,
- M' (d
717
X
6
ude AN)3-1:41954 i- 1
ecutr.Dn
I WOO:
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vu,? pr-rAi T-1 ed R m 'f,,- ~:,t ~P c V ~,ql J--'. T
Af
Ff t '[f rt! r, y V-i, W HoCl. ,nd M r w~d KUH ~~cl I 't"
P-Yr- t P.
pL-,I,fe CIT Cff CfjryO C411, CT!"n h, 4.r,- 4 r1l, -Y. CH.
CIT, CH CCH,
ari, c"
In-
r"Crygid frmn 100 ml moll face 10 g. P-PkCJT--
11CH~11'.1f.CHO "XT XI
p4
-tm"~
I~ii ~" ! -X~ 1 vn-:f,
2~- L
Vv
11, -nt
47
/, . I
bo~ 160-3*, m R7-8* (from (24191rligroinr'j. XX (I r I I"
10 mi. PtOll added drnpwisr to .1 mi. Njl.Jf,4) iti MCC
and tlip rwi-ndurl rrv- rod vi~lded 11 111 i io Ti 'A, -i- fin
ff-- FJOH F1 7
T'Ji
M )l VIT
nar-2 furiinc-Tv, , 1~ f~ 1 21
Finif 111.1t,ri -th _g 'f.
the r-lur rt~,Y,td f-- 1;(()If p-.- -r VI
plifirleel by vililimin; '.III ~-l
rr-iilUC tW!N? FtOITI P1011. YllllliTIf, V1, ~',2 4
11 Derl~.tives and n~bigti if p -moial!cv4ir
Virgim, I T W, r,nd-,v, -t
d,Ii,i --l i
~err prcpd rid tc-c I f- anti-
',]I th~ C,MIAS ji~,4 r
tiem than I The f,illowing comMs W~vrr llf-d
and min eff-rti,e filn gi-il
(11). inactive at M/IOWO; 2J-110(Cl~Cjl.c~,ll (11.1'.
4-W-V ~7 7.1r,ClrO!r
1""KI, 2 4-H()~2 4 if, ~ H 1.11::C~H 1C C) %,W C'I ili
.1,f~Pxw)u. TVz
4-HO cI .2-C,.11.,.C C) I C.1 1,C Cis F-_IV 1-
azlive a- WIN"), rZ.-il(AurHK~,__-.l'OJl '71).
tfilllok), at
,rM
un, h-~,; n
r- 71
'111 lb~ Cijcl~ ~~.s !r,TpviU! with ;tlrfirg -A rr~)i-
fil--
H,N. ~ilh 510 11cl. finAlhe .~Shcd ~Iln i
Et(,H.
2.4-PC,[2.4-IIICKO,t,;)C.14.(toill'Ic.ii.Co-F-t
2* 1H ydrog~.,aticn of 5 g. X in 250 ml. BtOAc cr~ I Oclo
Pd-C gm~e the Hs.14 compd (M), cnlmlc~s nmUes, m. ZOG-
I' (from ArOH). HydrolYsis of X1 With ;Lq. NZOH Pve
6,; 1, ~ " ;
from- C11104 widi'abs. m0fl, ~nl6r-
le,% decoingid. 212-3'. 1 (3 g,) and 2.9 -. plithuJic an-
hydride (X11) in 160 o71. MO.Ac let stand 21 hr:v. at room
temp.. tilt material filtered. and washtd with MOAc
afforded ML acid, dcccmpd. W-00* with ras evo4ttlo.'l.
bccoming solid, anti then m. 215-20'. K Et ester (3.6 g.)
ond 3 g. X11 in 60 mt. EtOAc let stand cvcrn~gght. the
i~tyst. prctdLwt fittcred, and w-ashtd with FtOAc g-ave 4.7
C, M, m. 179,90' (4ccompn.). Ma (I It.) healrd I hr.
-Ikt ZM' n-id rccrystd. yieMed V, m. 192-3" (front AcOll).
Beluoyllatioll Gf 15.3 g. I In aq. N.11CO2 gav-, 21) Fi. VIE, tn.
230-1" (I'mm MOU). P-IT0-CCH-.ClICJT,NIT..HCt (5
g-)and6OmI-PrOIItren'cd4 hrs, with dry lICl whilt!
Ing on the water hath, the ,min. cooled, file etyst. tnateri~-d
filtered. and washed Willi a little Pro"I gave 3 g, VIL 11C1.
in. 210' (deenmpit.). wMiam Brrt~~
34S
1954 ,
- J." -ti, t.-
ji W" ~ - -
c jt "O.-M,
t-C
v Wq
Synthesis and biological GA-rity of diphenyl aild indane
e"irtyatives. U~zliil, N T. Horvath. T N6rgTiai, ri
Y U94
and L nt Pluwu l,i,!
I
J 1- 1 4-5
4
dux is
4
fnrr A-4 M. II
m I! A '1,1! 13 2 4g ; ;11 ,
M. 2,1 ~a' (fr.,in A,OH H~aunz: ~~i III =i,h M
drvN iA, -1 41' 4
V1 J-h,
v! 2-.9- - -'- - ):~., rA. --;i~ i".11.
( 4 gc) ia 0 ml- dimaite treal--d witb 29.4 ml. 2M.
11.86, glveS 1.2 Cf. 4-ACOCH.C.',l,CJf-CrjCTfOH4 (Vrr*,,
cCJCrI1---,3 ttt-ed:ts, m. 1n-7' (f-m a!, ,V1 113
hc3teil witb 04) nil. AcOll givri 4.2~1 g1. mm, " ti it e !t-a
m. 117-18* (firnim FtOll) Reflimme, 2 S1 g VII Ith I!,
ml. Ac%O xives 2.0 R. 1. Tr~trn"t 121 z~ .4 110-CC11-
ThIC11:P0,11 (VM) kith 240 PCI, follo-d bv r-r--l
o, POC anA -f 121 g W1, in :Y'
j~" 64 IF. ii~ 'x mswr-gpwrcrnarl~ yel;cw Cty5faLq
M. IM-4",Umm liffrel"). P=ry I,.- if
41-Hydrary-5-cholenic acid and 3,3-hydraxy S-prepea-
"Ote ftm hyodeoxycbuUt arid. V_ az;d M.
" 1
CH 1Z
a
11~1. Chem-
isiry & InJuilry 1055. slpri -7-Me (1)
dirti)lmv, m. l6a-7' (ftow 9.7'
(e 2.07, CIICI*), (tog.), It) g. KOAc, and 10) mi. Ac,O
"'
boiled 45 min. Lrive 40
r Me 3,3-acetoxy-S-chutcnatc (U)
0
m, 155--6* (front EtOAc), -19.0' (c 21.14. C!ICI,): 1
hydrolyzed with alkali to 30-hydroxy-5-chofenic acid, !n.
235'. Analogoti-i acetrilysis of I dirn~_-ylate. m. 1i8-191
(from Fioll), In]',' 5,sri* (6 (Myjr), Cliel.), &~%Ve It. And
gave 30-extoxy-5-preg-
nen-20--one, m, Tile nim1cm6m of mqvtioll ill-'
volvcs himl. ucetuly~i, with itivcrsimi et C-3 arid Climi-,
nation of P-.%kC,11,SA)j1 fifull C-b U10 C-6.
Ire
TA
.4-M
.,Pig. men sugm. dulladva WM eltritttle d4waly.
N at w ms iw . ~ ch4flfe n, 19 5 5, 42, 5: F t.J. u -L- S! -I
Ind , N.,d;ijw,,t VII. ',Fl ---9f vfvvi: j ~-,, r
t!,~ ~)Ilowine t-d c,,-4;~5tanc or tum,:11- "W
er'
Retwity I 2-f5opmpylid k.-
furanme (m p 131-132', from N~i1wenc, ~u
ClIC1, - 8,0' viLiter) and I O-Li~f likircir--thyl .rm4T lfj)- 1 6-
dpox~ i)-ii)ariitit~)I-dihy(iriclilotide ~m p 241(1- -241 ' cr y it from
dilute, ethanul , jn'~.' 18-46' vwatcr~ ~GerniAa;
I e-6 SI ANI-BY
100)
CZECHOSLOVAKIA/General Problems of Pathology - Tumors. T-5
JA,bs Jour Ref Zhur - Biol., No 1) 1958, 3135
Author Varga, L.
Inst
Title Synthesis of New Sugar Derivatives with Cytostatic Activity
Orig Pub Ceskoal. Farmac., 1957, 6, No 1, 16-20
Abstract A series of ethylenimine and dichlorethylamine derivatives
of sugars, and their structural congeners, were synthesi-
zed. Ethane and hexane derivatives, as well as acid ami-
des, in a dose of 50 mg/kg suppressed Geren and N-1 carci-
nomas in rats, Crocker sarcomas and Ehrlich ascites carci-
noma8 in mice. A glucofuran derivative was less effective.
A glucosamine derivative in a dose of 2 mg/kg also suppres-
sed the Geren sarcoma by 50% but the experimental animals
died from toxicity. The most interesting proved to be a
mannite derivative (compound BCM, the dichlorhydrate of 1,
6 bis-beta-chlorethyl-amino 1,6-deoxy-D- nnite).
Card 1/2
HUNGARY / Organic Chemistry. Natural Substances and G
0
Their Synthetic Analomues.
Abs Jour: Ref Zhur-Khimiya, No 18, 1958, 51o6l.
Author : Lasz
Inst :'ca emy of Sciences of Hungary.
Title :Synthesis of New Cytostatically Acting Derivatives
of Sugars,
Ori- Pub: Magyar tud, akad. Kern. tud. oszt. kozl., 1957, 9,
No 1, 93-101,
Abstract: In view of the fact that the knovin anticancer
dru-s possessinG cytoactive groups are strange to
the organism, i.e., do not participate in the ex-
change of the cell substances, the following
ethyleniniino-, 13 -chlorethylamino- and (S-dichloro-
dietbylamino-substitutes of sugar:3 viere syntheti-
zed: 1:2-isopropilidene-6-ethyleniriino-6-desoxy-
Card 119
50
HUNGARY Organic Chemistry. Natural Substances and G
Their Synthetic Analogues.
Abs Jour: Ref Zhur-Khimiya, No 18) 1958, 61o6l.
Abstract: meltin point 144 to 1450, [ 0\ ]20D = +28. 180
(viater~; bis-( 9-chloroethylamide) of D-glucosac-
charic acid CM Hl806N2C12 (VI), melting point IY2
to 17110, [-