Synthesis and Anticancer Activity of Novel 2-Phenylindole Linked Imidazolothiazole, Thiazolo-s-triazine and Imidazolyl-Sugar Systems

Novel functionalized 2-phenylindole derivatives, their derived imidazolethione and 1,2,4-triazinethione weresynthesized. The bicyclic compounds thiazoloimidazole and thiazolotriazine compounds in addition to their arylidinederivatives 5-8 were synthesized. Furthermore, a thioglycoside, as well as sugar hydrazone derivatives of theimidazolylindole system, were prepared. Some of the prepared compounds were screened against four cancer celllines and compounds 2, 3a and 10 showed high cytotoxic activities. The imidazolylindol-3-one derivatives 3a showedsignificant cytotoxic effect superior to the reference drug, doxorubicin, against breast adenocarcinoma cell line.

Synthesis and reactions of some pyridopyrimidine and thienopyridine derivatives for antiviral evaluation

Compounds 6-amino-4-[4-chlorophenyl]-2-thien-2-ylpyridine5-carbonitrile [2] and 4-[4-chlorophenyl]-6-thioxo-2-thien-2-yll,6-dihydropyridine-5-carbonitrile [9] were prepaied using 3-[4-chlorophenyl]-l-thien-2-ylpropenone [I] and malononitrile or cyanothioacetamide, respectively. Pyridine derivative 2 was in turn used as a precursor for preparation of some pyridopyrimidine and fused pyridopyrimidine derivatives 3-8. On the other hand, the pyridine derivative 9 was used in preparation of thienopyridine derivatives 10 and 11. Moreover, fusion of compound 11 with excess of benzoyl chloride ' afforded 4-[4-chlorophenyl]-2-phenyl-7-thien-2-yl-3H-pyrido [3,2:4,5] thieno[3,2-d] pyrimidin-4-one [12]

Anti - glucose regulated protein 78 [GRP78] antibody responses in Alum/ALM plus BCG vaccinee, visceral leishmaniasis, and Post Kala- azar Dermal leishmaniasis patients

The Glucose Regulated Protein 78 [GRP78] of Leishmania donovani is considered to be one of the potential Leishmania vaccine candidates. Using Enzyme-Linked Immunosorbent Assay [ELISA], we measured IgG antibody responses to GRP78 in 39 healthy Sudanese volunteers vaccinated with Leishmania Alum/ALM + BCG vaccine, 29 patients with visceral leishmaniasis [VL], and 26 patients with post kala-azar dermal leishmaniasis [PKDL]. There was, no significant statistical difference in plasma levels of GRP78 antibodies in immunized and control group [P=0.37]. Furthermore, no significant statistical difference in the levels of GRP78 antibodies in the pre and post vaccination plasma samples [P=0.60]. Plasma IgG levels to GRP78 was significantly higher in visceral leishmaniasis and PKDL patients compared with control group [P=0.00]. This study concludes that Alum/ALM vaccine does not induce a Th2 type of immune response. It also demonstrated clearly that VL and PKDL are associated with elevation of anti-GRP 78 antibodies and that GRP78 ELISA can be used to confirm diagnosis of Leishmania infections based on the clinical presentation

Reactions of, B-spiroepoxy-alkannans part IV+ New and facile synthesis of tetrahydric-naphthalin-2-01 derivatives for biological evaluation

Spirooctanones II react with acetoacetanilide to form tetrahydro-naphthalene derivatives IIIa,b, which react with phosphorus oxychloride to give the corresponding chloro derivatives IV. Compounds IV react with hydrazine hydrate, aniline, and hydroxylamine to give the corresponding compounds V, VI and VII, respectively. Compounds V condensed with aromatic aldehydes to give the corresponding hydrazones VIII

Reactions with spiroepoxy-alkanones. part III+ reaction of spirooctanones with dimethylamine aldehyde and then thiourea

Spirooctanones I react with dimethylamine at different conditions to give compounds II and III, and in the presence of aldehydes give IV. Compounds IV react with thiourea to give V, which undergoes cyclization with chloroacetic acid to give VI. Compounds VI condensed with dimethylamino-benzaldehyde to give VII. Some of the prepared compounds are biologically active

Synthesis and reactions of B-ketoanilides for biological evaluation

2-Arylidene cycloalkanones react with acetocetanilide to give the corresponding B-ketoanilides Ia-f which react with hydroxyl-amine and/or hydrazine hydrate in acetic acid to give respectively compounds III and compounds V. Compounds I also react with o-phenylene diamine and/or diethyl malonatethiourea to produce respectively compounds VI and compounds VIII. Chemical screening for the products are mentioned