Methyl indolenines (4a-c) and (5a-c) were prepared in high yield by a Fischer indole synthesis reaction of o,m-tolylhydrazine hydrochlorides (1a-b) with isopropyl methyl ketone (2) and 2-methylcyclohexanone (3) in acetic acid at room temperature. o,p- Nitrophenylhydrazines (1c-d) were reacted with 2-methylcyclohexanone (3) in acetic acid at reflux to give nitroindolenines (5d-e), while the attempted reactions of o,p-nitrohydrazines with isopropyl methyl ketone (2) in acetic acid were not successful. Compounds (1c-d) were reacted with isopropyl methyl ketone (2) in acetic acid/HCl to give 2,3,3-trimethyl-5-nitro-indolenine (4e) and 2,3,3-trimethyl-7-nitroindolenine (4d).

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Pseudopolyrotaxanes (PPR) consisting of -cyclodextrin rings and polyethylene glycol axes with end thymine groups have been synthesized and characterized successfully. Fluorescein (Fl) as a model drug was conjugated to the hydroxyl functional groups of cyclodextrin rings of PPR via ester bonds and PPR-Fl as the primary drug delivery system was obtained. Finally PPR-Fl was capped by hydrogen bonds between end thymine groups and a suitable complementary molecule such as polycitric acid, citric acid, or adenine. The aim of this work was to control the release of the fluorescein-cyclodextrin (Fl-CD) conjugates, as the secondary drug delivery systems, from PPR-Fl by controlling the noncovalent interactions between stoppers and thymine end groups. It was found that the rate of release of the Fl-CD from PPR-Fl could be controlled by pH and the ratio of citric acid or adenine to the PPR-Fl.

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Several derivatives of 6 amino 4 aryl 2 thioxo 1,2,3,4 tetrahydropyrimidine 5 carbonitriles were synthesized via Biginelli type reaction and tested for their anti proliferative activity on human breast cancer (MCF 7) and human colon carcinoma (HT29) cell lines. Malignant and non malignant cells were cultivated in RPMI medium and incubated with different concentrations of these pyrimidines. Cell viability was evaluated by MTT assay. Apoptotic cells were determined using DAPI (4' 6 diamidino 2 phenylindole) and propidium iodide staining of DNA fragmentation by flow cytometry (sub G1 peak). 6 Amino 4 (4 chlorophenyl) 2 thioxo 1,2,3,4 tetrahydropyrimidine 5 carbonitrile and 6 amino 4 [4 dimethy lamino)phenyl] 2 thioxo 1,2,3,4 tetrahydropyrimidine 5 carbonitrile decreased the viability of MCF 7 and HT29 cells, in contrast to L929 cells. These compounds induced a sub G1 peak inflow cytometry histo grams of treated cells indicating that apoptosis is involved in their toxicity.