http://chineseinput.net/에서 pinyin(병음)방식으로 중국어를 변환할 수 있습니다.
변환된 중국어를 복사하여 사용하시면 됩니다.
- 中文 을 입력하시려면 zhongwen을 입력하시고 space를누르시면됩니다.
- 北京 을 입력하시려면 beijing을 입력하시고 space를 누르시면 됩니다.
RISS 인기검색어
- 검색키워드
- 저자 : El-Faham, Ayman (검색결과 4 건)
- 무료
- 기관 내 무료
- 유료
-
Farooq, Muhammad,El-Faham, Ayman,Khattab, Sherine N.,Elkayal, Ahmed M.,Ibrahim, Mahmoud F.,Taha, Nael Abu,Baabbad, Almohannad,Wadaan, Mohammad A.M.,Hamed, Ezaat A. Asian Pacific Journal of Cancer Prevention 2014 Asian Pacific journal of cancer prevention Vol.15 No.18
Background: Valproic acid (VPA) is a potent anticancer and antiangiogenic agent. However, design and synthesis of chemical derivatives with improved antiangiogenic and anticancer activities are still necessary. In this study a library of novel derivatives of VPA was synthesized and tested. Methods: A human liver cancer cell line (HepG2) and a human normal embryonic kidney cell line (HEK 293) were exposed to various concentrations of VPA derivatives for 24 hours and cell viability was checked by MTT colorimetric assay. Anti-angiogenic properties were evaluated in transgenic zebrafish embryos. Results: N-valproylglycine derivatives suppressed survival almost 70% (p value 0.001) in HepG2 cells but only 10-12% in HEK 293 cells (p value 0.133). They also suppressed angiogenic blood vessel formation by 80% when used between $2-20{\mu}M$ in zebrafish embryos. Valproic acid hydrazides showed moderate level of anticancer activity by affecting 30-50% (p value 0.001) of cell viability in HepG2 cells and 8-10% in HEK293 cells (p value 0.034). Conclusion: The majority of compounds in this study showed potent and stronger antiangiogenic and anticancer activity than VPA. They proved selectively toxic to cancer cells and safer for normal cells. Moreover, these compounds inhibited developmental angiogenesis in zebrafish embryos. Based on the fact that liver is a highly vascularized organ, in case of liver carcinoma these compounds have the potential to target the pathological angiogenesis and could be an effective strategy to treat hepatocellular carcinoma.
-
Albatal, Mona,Ghani, Mohamad Abdul,El-Faham, Ayman,Al-Hazimi, Hassan M.,Hammud, Hassan H. Korean Chemical Society 2010 대한화학회지 Vol.54 No.4
마이크로웨이브 반응 장치 (Synthos 3000 Aton Paar, GmbH, 1400 W maximum magnetron)를 이용하여, diisopropylcarbodiimide (DIC)/와 1-hydroxybenzotriazoles (HOXt) (X = A or B)를 반응시켜서 amino acid hydrazide를 효율적으로 합성할 수 있는 반응 조건을 개발하였다. 일반적인 가열반응과 마이크로웨이브 반응을 반응 시간, 반응 조건 등을 비교하였을 때에, 마이크로웨이브 반응이 보다 효율적으로 진행되었으며, diisopropylcarbodiimide (DIC)와 1-hydroxybenzotriazole (HOBt) 반응에서보다는 diisopropylcarbodiimide (DIC)와 7-aza-1-hydroxybenzotriazole (HOAt)를 반응시켰을 때에 좋은 수율 (95 - 98%)로 얻어졌다. Here we describe a fast and rapid technique for preparation of amino acid hydrazide as well as peptide hydrazide derivatives using diisopropylcarbodiimide (DIC)/1-hydroxybenzotriazoles (HOXt) (X = A or B) under microwave irradiation employing a multimode reactor (Synthos 3000 Aton Paar, GmbH, 1400 W maximum magnetron). A comparison between conventional and microwave irradiation was described. The microwave methodology is rapid, convenient, proceeds under mild conditions. Diisopropylcarbodiimide (DIC)/7-aza-1-hydroxybenzotriazole (HOAt) always gave much better yield (95 - 98%) and purity than diisopropylcarbodiimide (DIC)/1-hydroxybenzotriazole (HOBt).
-
Synthesis and Aminolysis of N,N-Diethyl Carbamic Ester of HOBt Derivatives
Sherine Nabil Khattab,Seham Yassin Hassan,Ezzat Awad Hamed,Fernando Albericio,Ayman El-Faham 대한화학회 2010 Bulletin of the Korean Chemical Society Vol.31 No.1
The reaction of N,N-diethyl carbamates of 1H-[1,2,3]triazolo[4,5-b]pyridin-1-ol (4-HOAt) 7, 3H-[1,2,3]triazolo[4,5-b]pyridin-3-ol (7-HOAt) 8, 1H-benzo[d][1,2,3]triazol-1-ol (HOBt) 9, 6-chloro-1H-benzo[d][1,2,3]triazol-1-ol (Cl-HOBt) 10, 6-(trifluoromethyl)-1H-benzo[d][1,2,3]triazol-1-ol (CF3-HOBt) 11, and 6-nitro-1H-benzo[d][1,2,3]triazol-1-ol (NO2-HOBt) 12 with morpholine and piperidine in CH3CN underwent acyl nucleophilic substitution to give the Corresponding carboxamide derivatives. The reactants and products were identified by elemental analysis, IR and NMR.We measured the kinetics of these reactions spectrophotometrically in CH3CN at a range of temperatures. The rates of morpholinolysis and piperidinolysis were found to fit the Hammett equation and correlated with σ-Hammett values.The values were 1.44 - 1.21 for morpholinolysis and 1.95 - 1.72 for piperidinolysis depending on the temperature. The Brønsted-type plot was linear with a βlg = −0.49 ± 0.02 and −0.67 ± 0.03. The kinetic data and structure-reactivity relationships indicate that the reaction of 9-12 with amines proceeds by a concerted mechanism. The deviation from linearity of the correlation ΔH# vs. ΔS# and plot of logkpip vs. logkmorph and Brønsted-type correlation indicate that the reactions of amines with carbamates 7 and 8 is attributed to the electronic nature of their leaving groups
-
Synthesis and Aminolysis of N,N-Diethyl Carbamic Ester of HOBt Derivatives
Khattab, Sherine Nabil,Hassan, Seham Yassin,Hamed, Ezzat Awad,Albericio, Fernando,El-Faham, Ayman Korean Chemical Society 2010 Bulletin of the Korean Chemical Society Vol.31 No.1
The reaction of N,N-diethyl carbamates of 1H-[1,2,3]triazolo[4,5-b]pyridin-1-ol (4-HOAt) 7, 3H-[1,2,3]triazolo[4,5-b]pyridin-3-ol (7-HOAt) 8, 1H-benzo[d][1,2,3]triazol-1-ol (HOBt) 9, 6-chloro-1H-benzo[d][1,2,3]triazol-1-ol (Cl-HOBt) 10, 6-(trifluoromethyl)-1H-benzo[d][1,2,3]triazol-1-ol ($CF_3$-HOBt) 11, and 6-nitro-1H-benzo[d][1,2,3]triazol-1-ol ($NO_2$-HOBt) 12 with morpholine and piperidine in $CH_3CN$ underwent acyl nucleophilic substitution to give the corresponding carboxamide derivatives. The reactants and products were identified by elemental analysis, IR and NMR. We measured the kinetics of these reactions spectrophotometrically in $CH_3CN$ at a range of temperatures. The rates of morpholinolysis and piperidinolysis were found to fit the Hammett equation and correlated with $\sigma$-Hammett values. The values were 1.44 - 1.21 for morpholinolysis and 1.95 - 1.72 for piperidinolysis depending on the temperature. The $Br{\phi}$nsted-type plot was linear with a $\beta_lg = -0.49 \pm 0.02$ and $-0.67 \pm 0.03$. The kinetic data and structure-reactivity relationships indicate that the reaction of 9-12 with amines proceeds by a concerted mechanism. The deviation from linearity of the correlation ${\Delta}H^#$ vs. ${\Delta}S^#$ and plot of $logk_{pip}$ vs. $logk_{morph}$ and $Br{\phi}$nsted-type correlation indicate that the reactions of amines with carbamates 7 and 8 is attributed to the electronic nature of their leaving groups.
DBpia연관 검색어 추천
이 검색어로 많이 본 자료
활용도 높은 자료
