Novi steroidni derivati sintetizirani iz 3betha-hidroksiandrosten-17-ona

In this study, we synthesized some new substituted steroidal derivatives using 3betha-hydroxyandrosten-17-one (dehydroepiandrosterone) as starting material. The synthesized steroidal derivatives 1-11 were evaluated for their androgenic-anabolic activities compared to testosterone as positive control. Details of the synthesis, spectroscopic data and toxicity (LD50) of synthesized compounds are reported.U radu je opisana sinteza novih steroidnih derivata 1-11 koristeći 3betha-hidroksiandrosten-17-on (dehidroepiandrosteron) kao početnu supstanciju. Androgeno-anaboličko djelovanje tih spojeva uspoređivano je s djelovanjem testosterona kao pozitivnom kontrolom. Navode se detaljni sintetski postupci, spektroskopska karakterizacija i podaci o toksičnosti (LD50)

The contingent factors that affect the use of performance measurement systems in the Egyptian medium and large sized manufacturing companies

EThOS - Electronic Theses Online ServiceGBUnited Kingdo

Remote Sensing Satellites Planning System

A Remote Sensing Satellites Planning system (RSSP) for satellite constellations is responsible for managing these satellites by assigning the imaging tasks to each satellite in the constellation such that the loads are balanced and the resources are well used. The proposed system can be used with heterogeneous constellations that consist of satellites whose different specifications, different orbits' types and/or different payload types. This problem is a combinatorial optimization NP-hard problem modeled in this paper as a Constraint Satisfaction Problem using the Constraint Programming Technique. The output plan is obtained using one of three objective functions (gain maximization, area maximization, and image quality maximization) using four search algorithms (simulated annealing, hill climbing, tabu search and late acceptance) and different planning horizons (one track, one day and one month)

Investigation of Growth Inhibitory Effects of cyclo (Nα-pyrido)-bis-[(L-valinyl)-L-ornthenyl acid hydrazide] on Various Cancer Cells as well as in vitro VEGFR-2 Kinase Inhibition

328–332During the current work, we synthesized a new peptide derivative; 4,13-diisopropyl-2,5,12,15-tetraoxo-3,6,11,14-tetraaza-1(3,5)-pyridinacyclopentadecaphane-7-carbohydrazide. The prepared hydrazide was investigated for its in vivo as well as in vitro anticancer effects. Results revealed that this derivative has a great potential against 6 cancerous cell lines. Furthermore, the highest effect was obtained against HT1080 and HeLa cells, where the compound showed 7.4- and 15.1-folds increased activity against them, respectively. Additionally, the compound seems to exert its potential anticancer effect by affecting the kinase enzyme VEGFR-2. Finally, the compound showed promising results when tested in in vivo against prostate cancer developed animal models

Anti-VEGFR-2 Kinase Effects of Cyclo (Nα-dinicotinoyl)-bis-[(L-valinyl)- L-lysine] and its Anticancer Activities Against Different Cancer Cell Lines

The current work aimed at preparing a cyclo (Nα-dinicotinoyl)-bis-[(L-valinyl)-L-lysine] from previously established synthetic routs. The derivative was investigated for its potential anticancer activities as well as its possible mechanism of action. The prepared compound showed variable anticancer activities against all tested cell lines. Furthermore, it showed very promising activities in terms of obtained IC50 values compared to known used drugs. The mechanism of action studies showed that the prepared tripeptide may act on cancerous cells through its inhibitory action on tyrosine kinase pathway. Animal model experiments proved the potential of the synthesized tripeptide as an anticancer agent against PC3 cancer cells

Antimicrobial Activities of some Synthesized Cyclo (Nα-dinicotinoyl) [L-phenylalanyl-L-leucine]Pentapeptide Candidates

71-76Some of cyclo (Nα-di-nicotinoyl)[L-phenylalanyl-L-leucine]pentapeptides3-6 has been synthesized starting from bis- (1-carboxy-2-substituted)-3,5-diaminocarbonyl)pyridine 3 and N,N-bis-(1-hydrazonyl-2-substituted)-3,5 diaminocarbonyl) pyridine 2. Treatment of 1 or 2 afforded the corresponding bis-ester derivative 3, which was hydrolyzed with sodium hydroxideto give bis-acid 4. Cyclization of bis-acid 4 with L-dibasic amino acid methyl esters, afforded the corresponding macrocyclic methyl esters 5a,b, respectively. Finally, hydrazonolysis of 5a,b with hydrazine hydrated in refluxing methanol afforded macrocyclic pentapeptide hydrazides 6a,b, respectively. Some of these compounds exhibited antimicrobial activities comparable with Chloramphenicol and Fusidic acid as reference drugs

Cyclo (Nα-dinicotinoyl)-bis-[(L-valinyl)-L-lysinyl acid hydrazide]: Assessment of its Role in Cancer and Kinase Activity Inhibition

292–296Current research aimed at evaluating the in vitro as well as in vivo anticancer activities of a newly synthesized peptide hydrazide; i.e. 4,14-diisopropyl-2,5,13,16-tetraoxo-3,6,12,15-tetraaza-1(3,5)-pyridinacyclohexadecaphane-7-carbohydrazide. The hydrazide was synthesized from methyl 4,14-diisopropyl-2,5,13,16-tetraoxo-3,6,12,15-tetraaza-1(3,5)-pyridinacyclohexadecaphane-7-carboxylate 2 by acting of hydrazine hydrate. It showed significant anticancer effects against different tested cell lines, where cervical, breast, liver, colon, prostate, brain, fibrosarcoma, leukemia and melanoma cell lines were the most affected cell types. The prepared derivative also inhibited VEGF-2 kinase enzyme significantly and exhibited an in vivo tumorigenic effects in mice model

Evaluation of in vitro and in vivo Cytotoxic Activities and Kinase Inhibition of Newly Synthesized Cyclo (Nα-Dinicotinoyl)-Bis-[(L-Valinyl)-L-Lysine Methyl Ester]

222-225Cancer is a major risk disease affecting human survival. The pharmaceutical companies are continuing searching for new drug candidates with promising anticancer activities, and reduced side effects. The current work aimed at synthesized a new tripeptide with potential pharmacological properties. L-Valine methyl ester was used to prepare cyclo (Nα-dinicotinoyl)-bis-[(L-valinyl)-L-lysine methyl ester. The new compound revealed promising in vitro cytotoxic activities against different neuroblastoma, cervical carcinoma, fibrosarcoma as well as hepatocellular carcinomas. Furthermore, we also found that the obtained IC50 of the compound decreased by about 50% during its in vivo anti-prostate cancer evaluation. Furthermore, the mechanism of action studies proposes that the new prepared derivative affects cancer cells trough the inhibition of VEGFR-2 kinase enzyme