Synthesis and pharmacological screening of certain substituted tetrahydropyrido [4,3-b] quinolines and pyrazole [4,3-c] quinolines

The synthesis of two series of annulated quinoline derivatives III and IV is presented. Pyrazolo [14,3-c] quinoline derivatives [IV] were also obtained by a newly reported rearrangement reaction [17]. The analgesic antipyretic as well as anti-inflammatory activities of 7-chloro-2 [benzothiazol-2-yl]-4 [2N-ethylamino] ethyl]-2H-pyrazolo [4,3-c] quinoline [IV6], 7-chloro-2 [benzothiazol-2-yl]-4 [2 N-propylamino] ethyl]-2H-pyrazolo [4,3-c] quinoline [IV6], 7-chloro-2 [benzothiazol-2-yl]-4[2 N-propylamino] ethyl]-2H-pyrazolo [4, 3-c] quinoline [IV12], 7-chloro-2 propyl-1,2,3,4-tetrahydropyrido [4,3-b] quinoline [III7] and 7-chloro-4 [2[N-ethylamino] ethyl]-2[4-hydroxy-6-methylpyrimidin-2-yl]-2H-pyrazolo [4,3-c] quinoline [IV3] have been investigated

Synthesis and antitumor activity of some substituted pyrimidines

The synthesis, in vitro antitumor and antibacterial activity of 2-amino-4- [amino or substituted amino]-6-[3,4, 5-trimethoxybenzoylamino] pyrimidines [2-10] and of 4-[amino or substituted amino]-6-methyl-2- [3,4,5-trimethoxybenzoylamino] pyrimidines [11-18] was described. Compounds 7 and 9 showed significant cytotoxic activity against Ehrlich ascites tumor cells, whereas compounds 5, 6 and 7 showed considerable antibacterial effect

N1, N3-diarly sulfonylureas as possible anticancer agents

This study described the synthesis of a number of sulofenur thiadiazole analogues with structural modification of the aryl moiety of the sulfonamide portion of the diaryl sulfonylureas. Two different methods were adopted in order to prepare the target compounds. The new compounds were evaluated for in vitro cytotoxic activity. Two compounds showed 100% activity against Ehrlich ascites tumor cells

Synthesis of some 4-substituted-pyrimidinylaminophenyl-6-aryl-1,2,5,6-tetrahydro-2-thioxopyrimidine derivatives as possible antimicrobial agents

A novel series of 4-substituted-pyrimidinylaminophenyl-6- aryl -1, 2, 5, 6-tetrahydro-2-thioxopyrimdines was synthesized. Treatment of 2- amino-4- chloro-6- methyl-pyrimidine [Ia] with p-aminoacetophenone afforded the corresponding key intermediate [II]. The latter was reacted with a number of aryl aldehydes to yield the chalcone analogues [III] which undergo cyclocondensation with thiourea to furnish the target compounds [IV]. Preliminary antimicrobial screening showed that some of these novel thioxopyrimidines posses moderate activity against certain gram positive bacteria

Synthesis and mass spectral studies of some 1- [2-benzimidazolyl] or [6-methyl-4 [1H] -pyrimidinon-2-yl] -5-substituted phenyl-3-methylpyrazoles

New 1-[2-benzimidazolyl] 5-substituted phenyl-3- methylpyrazoles [IV] and 1-[6-methyl-4 [1H] -pyrimidinon-2-yl]-5-substituted phenyl-3- methylpyrazoles [V] have been synthesized by the condensation of beta- diketones [III] and 2-hydrazinobenzimidazole [I] or 2-hydrazino-6- methyluracil [II], respectively. Bromination study of IV and V in Br2/ACOH has revealed that electrophilic attack of bromine occurs in pyrazole ring at position 4 and in uracil ring at position 5. The general spectral fragmentation mode of these compounds has been studied

Synthesis of certain 9- [substituted amino] acridines potential antitumor agents

9-aminoacridine [I] was converted to variety of 9-N-heterocyclic IIIa,b, N-methylcarbamido Vc-g, ureido VI and hydroxyureido IX derivatives in connection with a program synthesizing potential antitumor agents derived from acridine. Representative examples of the products were tested for in vitro antitumor activity against Ehrlich ascites cells. Two products showed perspective activities