X-ray structural analysis and antitumor activity of new salicylic acid derivatives

This Thesis project is going to be situated in my home town Östersund, 600 kilometers north from Stockholm.It´s a small town with 60 000 people and it is the only city of the region Jämtland in Norrland, Sweden.In the city centre of Östersund there is one existing bus terminal station where the buses arrive with people from the entire region.The task for this Thesis project is to rebuild the existing bus station in Östersund where the actual terminal building is going to be completely demolished and the entire block within the current bus stops is going to be rearranged.The topography of the terminal area is now dividing the regional buses that arrives on the upper level from the city buses that stops at the lower level. Therefore the main challenge of the new proposal is how one would strengthen the junction between these two flows of people and how a new architecture could enable the encounter between the countryside and the urban city.Detta examensprojekt kommer att vara belägen i min hemstad Östersund, 600 kilometer norr om Stockholm. Det är en liten stad med 60 000 personer och det är den enda staden i regionen Jämtland, Norrland. I centrum av Östersund finns en befintlig bussterminalen där bussarna anländer med folk från hela regionen. Uppgiften för detta projekt är att bygga om den befintliga busstationen i Östersund topografin på terminalområdet i dagsläget separerar de regionala bussarna som anländer på den övre nivån från stadsbussarna som stannar på en lägre nivå. Den största utmaningen i det nya förslaget är hur man istället skulle kunna stärka förbindelsen mellan dessa två flöden av människor och hur en ny arkitektur kan möjliggöra mötet mellan glesbyggd och den urbana staden

Synthesis and biological evaluation of some 17-picolyl and 17-picolinylidene androst-5-ene derivatives

Starting from dehydroepiandrosterone (1) 17-picolyl (2), 17-picolinylidene (7), 17-picolinylidene-16-one (10 and 11), and 17-picolyl-16-one (15) derivatives of androst-5-ene were synthesized in one, two, four and five steps respectively. By the Oppenauer oxidation or dehydration of 2, 7, 10, and 11 with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ), the corresponding A and B ring modified derivatives 3, 5, 6, 8, 9, and 12-14 were obtained. The structure of 2 was unambiguously proved by the appropriate X-ray structural analysis. Compounds 3, 5,9,12-14 showed inhibitory activity against the enzyme aromatase. Antibacterial activity toxicity to brine shrimp Artemia salina, antitumor activity against three tumor cell lines (human cervix carcinoma HeLa cells, human melanoma FemX cells, and human myelogenous leukemia K562 cells) and toxicity against peripheral blood mononuclear cells were evaluated. Three tested compounds, namely 11, 13, and 15, showed strong activity against all three cell lines, the IC50 values being in the range of 4-10 mu M. (c) 2006 Elsevier Inc. All rights reserved

Antioxidant and cytotoxic activity of mono- And bissalicylic acid derivatives

A simple synthesis of mono- and bis-salicylic acid derivatives 1-10 by the transesterification of methyl salicylate (methyl 2-hydroxybenzoate) with 3-oxapentane-1,5-diol, 3,6- dioxaoctane-1,8-diol, 3,6,9-trioxaundecane-1,11-diol, propane-1,2-diol or 1-aminopropan- 2-ol in alkaline conditions is reported. All compounds were tested in vitro on three malignant cell lines (MCF-7, MDA-MB-231, PC-3) and one non-tumor cell line (MRC- 5). Strong cytotoxicity against prostate PC-3 cancer cells expressed compounds 3, 4, 6, 9 and 10, all with the IC50 less than 10 μmol/L, which were 11-27 times higher than the cytotoxicity of antitumor drug doxorubicin. All tested compounds were not toxic against the non-tumor MRC-5 cell line. Antioxidant activity of the synthesized derivatives was also evaluated. Compounds 2, 5 and 8 were better OH radical scavengers than commercial antioxidants BHT and BHA. The synthesized compounds showed satisfactory scavenger activity, which was studied by QSAR modeling. A good correlation between the experimental variables IC50 DPPH and IC50 OH and MTI (molecular topological indices) molecular descriptors and CAA (accessible Connolly solvent surface area) for the new compounds 1, 3, and 5 was observed