Title:
Synthesis & characterization of ru(ii) , hg(ii) , pd(ii) & cu(i) with
N,n-bis[diphenylphosphine]-1-naphthylamine derivatives
/ by Akram A. Almejled ; supervised by Dr. Harbi Al-Masri. Ru(II) و Hg(II) و Pd(II) و Cu(I) اصطناع وتشخيص لمعقدات
مع مشتقات الليجند ن,ن-ثنائي(ثنائي فنل فوسفين)-1-نافثيل امين
Ru(II) و Hg(II) و Pd(II) و Cu(I) اصطناع وتشخيص لمعقدات
مع مشتقات الليجند ن,ن-ثنائي(ثنائي فنل فوسفين)-1-نافثيل امين
Ru(II) و Hg(II) و Pd(II) و Cu(I) اصطناع وتشخيص لمعقدات
مع مشتقات الليجند ن,ن-ثنائي(ثنائي فنل فوسفين)-1-نافثيل امين
Author:
Almejled, Akram A., author.
al-Masri, Harbi, supervisor.
Al al-Bayt University (Mafraq , Jordan). Faculty of Science. Department of Chemistry.
General Notes:
Thesis (M.Sc. in Chemistry)--Al al-Bayt University (Mafraq, Jordan), Faculty of Science, Department of Chemistry, 2019
Includes bibliographical references and index.
.
الليجندات ( 1-8 ) تم اعادة تحضيرها استنادا الى الطريقة المنشورة . تفاعل الليجاند 1 مع كمية مساوية من النحاسوز في خليط من الاسيتونايترايل وكلوريد الميثان لانتاج المعقد 9 . من خلال تفاعل الليجندات 5 و 6 مع كمية مساوية من الروثنيوم الدايمر في خليط من التيتراهايدروفيوران و كلوريد الميثان لانتاج المعقدات 10 و 11 . غلي الليجند 1 مع كلوريد البلاديوم في كلوريد الميثان لانتاج الدايمر 12 , والذي نتج عن الاكسدة والتميه اثناء تحضير الليجاند 1 لانتاج المركب 13 .
تفاعل الليجندات 1 و 4 مع ايوديد الزئبق في التيتراهايدروفيوران لانتاج 14 و 15 على التوالي .
تم تشخيص واثبات التركيب الجزيئي للمركبات 9 – 15 بواسطة التحليل الطيف الرنين المغناطيسي النووي متعدد النواة ( 1H , 13C , 31P و 77Se ) والاشعة تحت الحمراء , كذالك اثبات المعقدات 1 , 9 , 12 و 13 بواسطة الاشعة السينية احادي البلورة .
The ligands C10H7-1-N(PPh2)2 (1), C10H7-1-NH(PPh2) (2), C10H7-1-N(P(E)Ph2)2 [E = S (3), Se (4)], C10H7-1-N(P(E)Ph2)(PPh2) [E = S (5), Se (6)], and C10H7-1-NH(P(E)Ph2) [E = S (7), Se (8)] were resynthesized by the published method described in the literature .
The reaction of ligand 1 with two equivalents of CuI in a mixture of acetonitrile and methylene chloride resulted in the formation of octahedron Cu4I4[1]2 complex (9). Upon the reaction of the ligands 5 and 6 with [Ru(CO)3Cl2]2 in equimolar ratio in a mixture of tetrahydrofuran and methylene chloride the hexa-coordinated complexes of Ru(CO)2Cl2[5] (10) and Ru(CO)2Cl2[6] (11) were obtained .
Refluxing of ligand 1 with PdCl2(COD) in CH2Cl2 afforded the chloro-bridged dimer di-µ-chlorobis[diphenyloxophosphino]dipalladium(II) (12), which arose from an oxidation and hydrolysis during the preparation of ligand 1 to produce 1,1,2,2-tetraphenyldiphosphine dioxide, Ph2P(O)-P(O)Ph2 (13) instead of ligand 1. The reactions of the ligands 1 and 4 with mercury(II)iodide in equimolar ratio in tetrahydrofuran afforded HgI2[1] (14) and HgI2[4] (15), respectively.
Compounds 9-15 were identified and characterized by multinuclear NMR spectroscopy (1H, 13C, 31P, 77Se NMR) and IR. Crystal-structure determinations were carried out for 1, 9, 12 and 13..
The electronic version is available in theses database \\ University of Jordan.
Includes abstracts in Arabic and English.
Subject:
Chemistry.
Polymers.
Polymer Sciences.
Dissertation Note:
Thesis (M.Sc. in Chemistry)--Al al-Bayt University (Mafraq, Jordan), Faculty of Science, Department of Chemistry, 2019
Physical Description:
1CD-ROM : PDF.
Publication Date:
2019.
Title:
Synthesis and activation of bitter taste receptor 14 (tas2r14) agonists – an approach for assigning its active site / by Hothyfah Rushdi Mohammad Kittaneh ; supervised by Prof. Dr. Rafik Karaman. تصنيع وتفعيل طعم المر لمستقبلات 14 (TAS2R14) - نهج لتعيين موقعها النشط
تصنيع وتفعيل طعم المر لمستقبلات 14 (TAS2R14) - نهج لتعيين موقعها النشط تصنيع وتفعيل طعم المر لمستقبلات 14 (TAS2R14) - نهج لتعيين موقعها النشط
Author:
Kittaneh, Hothyfah Rushdi Mohammad, author.
Karaman, Rafik, supervisor.
Al-Quds University (Jerusalem, Palestine). Faculty of Science and Technology. Department of Chemistry.
General Notes:
Thesis (M. Sc. in Applied Industrial Technology)-- Al-Quds University (Jerusalem, Palestine), Faculty of Science and Technology, Department of Chemistry
, 2017.
Includes bibliographical references and index.
Sensing potentially harmful bitter substances in the oral cavity is achieved by a group of ~25 receptors, named TAS2Rs, which are expressed in specialized sensory cells and recognize individual but overlapping sets of bitter compounds. The receptors differ in their tuning breadths ranging from narrowly to broadly tuned receptors. One of the most broadly tuned human bitter taste receptors is the TAS2R14 recognizing an enormous variety of chemically diverse synthetic and natural bitter compounds, including numerous medicinal drugs. This suggests that this receptor possesses a large readily accessible ligand binding pocket. To allow probing the accessibility and size of the ligand binding pocket. Mefenamic acid (2-(2,3-dimethylphenyl)aminobenzoic acid) and diclofenac (2-(2,6-dichloranilino) phenylacetic acid) have been identified as novel TAS2R14 agonists in a recent in silico screening of agonists and confirmed by functional assays, a previously identified TAS2R14 agonist. Benzoin (2-hydroxy-1,2-di(phenyl)ethanone), which represents the most simple aromatic hydroxyl ketone and is a naturally in bitter almond oil, also belongs to TAS2R14 agonists. Bad contacts were observed between the hydrogen of the ligand alkoxy groups and the backbone Il2627.35, diclofenac derivatives cannot be accommodated in the binding pocket because of seteric hindrance. The resulting mefenamic acid benzyl ester retained agonistic properties, although the lack of receptor activation below a concentration of 10 μM indicates reduced potency. for both benzoin derivatives receptor responses already at concentrations of 10 μM, whereas the necessary concentration of unmodified benzoin required to activate TAS2R14 was ~10-fold higher. Mefenamic acid and diclofenac show an intramolecular H-bond between the alkoxy group and the aniline nitrogen, not present in the benzoin structure. Different derivatives alkyl/ benzyl of diclofenac, mefenamic acid and benzoin were synthesized and tested against TAS2R14. The derivatives with global minima with the substituent positioned far from the core of the compound skeleton structure (aniline nitrogen or carbonyl group), such as mefenamic acid hexyl, mefenamic acid decyl esters, benzoin benzyl and benzoin hexyl ethers, cause the activation of TAS2R14 to a variable extent, while the compounds with global minima for which substituent is placed near the structural core of the compound, such as in diclofenac derivatives, did not activate TAS2R14. Therefore, the difference between the mefenamic acid and benzoin derivatives on the one hand and the diclofenac derivatives on the other hand can be attributed to steric effects.
The electronic version is available in theses database \\ University of Jordan.
Includes abstracts in Arabic and English.
Subject:
Organic compounds
Organic compounds -- Industrial applications.
Dissertation Note:
Thesis (M. Sc. in Applied Industrial Technology)-- Al-Quds University (Jerusalem, Palestine), Faculty of Science and Technology, Department of Chemistry
, 2017.
Physical Description:
CD-ROM1 : PDF.
Publication Date:
2017.
Title:
Synthesis and anticancer activity
of novel pyridoquinoxaline derivatives
/ by Ala’a Saeed Tabaza, Supervised by Prof Dr.Yusuf Al-Hiari.
تصنيع و دراسة الخصائص المضاده للسرطان لمركبات بيريدوكوينوكسالين جديده
تصنيع و دراسة الخصائص المضاده للسرطان لمركبات بيريدوكوينوكسالين جديده
تصنيع و دراسة الخصائص المضاده للسرطان لمركبات بيريدوكوينوكسالين جديده
Author:
Tabaza, Ala’a Saeed, author.
al-Hiari, Yusuf, supervisor.
abu-Dahab, Rana Mohammed, So-supervisor.
The University of Jordan. School of Pharmacy. Department of Pharmaceutical Sciences.
General Notes:
Thesis (M.Sc in pharmaceutical Sciences)--The University of Jordan (Amman, Jordan), School of Pharmacy
, Department of Pharmaceutical Sciences, 2019.
Includes bibliographical references and index.
In a world where cancer continues to be a major health problem the urgency continues to find new effective treatments. This work aims at preparing new tetrahybridpyridoquinoxalines system (PQs) originating from fluoroquinolone (FQs) derivatives and tests their anticancer activity. Synthesis of the new compounds of the PQ series was carried out by reacting 1-cyclopropyl-6-fluoro-8-nitro-4- oxo-1,4-dihydroquinoline-3-carboxylic acid with L-proline, 3 and 4-hydroxy proline derivatives (compounds 2 (a-f)), followed by reductive cyclization to yield compounds 3 (a-f). Compounds 2a and 3a gave favorable activities on MCF-7 (5.9 M and 0.9M respectively), while the hydroxy derivatives almost lost activity on all tested cells. Although PQs showed chief activity against MCF-7, compound 3a in particular super-passed the reference Cisplatin with IC50 value of 22.9M. Due to the fact that activity of PQs and precursor FQs was correlated to increased lipophilicity, lipophilic FQ series 10-11(a-b) were prepared by direct reaction of 1-cyclohexyl-6-fluoro-8-nitro-4- oxo-1,4-dihydroquinoline-3-caroxylate with chloro or flouro aniline followed by ester hydrolysis 10(a,b) and reduction to yield the amine compounds 11(a,b). All the FQs 10-11(a-b) showed very excellent activity against all tested cell lines (MCF-7, MDA-MB-231 and DU145) with IC50 values below 20M. All compounds were also tested for their adhesion and invasion potential; only FQs showing comparable or supra anti-adhesion and anti-invasion activity compared to the reference Quercitin. The difference in pattern of anticancer activity and broadness of activity between FQs and PQs could be related to extra nitro or amino group on C-8 suggesting new different mechanism for each class. Structure activity relationship (SAR) and quantitative structure activity (QSAR) reveal that planarity due to fused polycyclic system and lipophilicity were essential requirements for anticancer PQs, whereas high number of H-B (hydrogen bond) and increased number of chelators in addition to lipophilic balance are the major requirements for anticancer FQs.
In conclusion this research opens the door for new wide spectrum potential anticancer PQs (3a and f) and FQs10-11 (a,b) that have better bioavailability, and are cheaper.
.
في عالم لا يزال فيه السرطان يمثل مشكلة صحية كبيرة ، تستمر الحاجة الملحة لإيجاد علاجات جديدة فعالة. يهدف هذا العمل إلى إعداد مركبات بيريدوكوينوكسالين مشتقه من الفلوروكوينولونز ودراسة نشاطها في مكافحة السرطان باستخدام طريقة SRB في المختبر. بالمقارنة مع مفعول دواء السرطان المسجل سيسبلاتين تم تقييم نشاط المركبات الجديدة من الفلوروكينولونات FQs و ال بيريدوكوينوكسالين PQ في تثبيط التكاثر الخلوي السرطاني على لائحة من خلايا سرطان الثدي (MCF7 و MDA-MB-231) ، سرطان البروستات (DU 145)، وكذلك على خلايا الرباط اللثوي الليفي الطبيعي لدراسة مدى أمان هذه المركبات الجديدة.
تمت عمليه تحضير مجموعه ال PQ من خلال تفاعل اضافه الحمض الأميني البرولين الى حلقه الفلوروكوينولون متبوعا بتفاعل اختزال لتكوين المشتق الرباعي الحلقات. تبين بالفحص اليبولوجي ان المركب 2a و المركب 3a يمتلكان أقوى خصائص مضاده للسرطان مقارنة بالدواء سيسبلانين (وصلت قيمه IC50 0.9173 و 5.032 ميكرومولار على التوالي). أما مجموعه المركبات فلوروكوينولون فتم تحضيرها باضافه كلورو او فلورو انلين الى حلقه الكوينولون ثم عمل اختزال للمركب. و قد أظهرت جميع المركبات من هذه المجموعه 10-11(a-b)خصائص مقاومه للسرطان على جميع الخلايا المفحوصه (MDA-MB-231, MCF7, DU 145) مع قيم IC50 أقل من 20 ميكرومولار. تم فحص المركبات أيضا ضد مقاومه غزو الخلايا السرطانيه و التصاقها و أظهرت مشتفات الكلورو و فلورو انلين خصائص مثبطه لغزو خلايا السرطان المفحوصه. بناء على دراسات ربط الفعاليه بالبناء الجزيئي فانه من المقترح أن هذه المركبات تقوم بالارتباط بالانزيم توبوايسوميريز2 و بال DNA مع ارتباط معدن مثل الحديد او المغنيزيوم, يطرح هذا ضروره وجود مجموعات قادره على الارتباط مع المعادن كجزء ضروري حتى تعطي هذه المجموعه من المركبات التأثير المضاد للسرطان. في الختام ، يفتح هذا البحث الباب أمام مضادات السرطان المحتملة ذات الطيف الواسع, لديها توفر بيولوجي أفضل ، ورخيصة ، و لديها سميه اقل مقارنه بالادويه المستخدمه حاليا في علاج السرطان.
The electronic version is available in theses database \\ University of Jordan.
Includes abstracts in Arabic and English.
Subject:
Pharmacology
Drug interactions.
Cancer -- Treatment.
Breast -- Cancer.
Drugs -- Structure activity relationships
QSAR (Biochemistry)
Organic compounds -- Synthesis.
Breast -- Cancer -- Treatment.
Breast -- Cancer -- Prevention.
Dissertation Note:
Thesis (M.Sc in pharmaceutical Sciences)--The University of Jordan (Amman, Jordan), School of Pharmacy
, Department of Pharmaceutical Sciences, 2019.
Physical Description:
1CD-ROM : PDF.
Publication Date:
2019.
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