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Jo, Nam Hyun,Kim, Jung Young,El‐,Gamal, Mohammed I.,Choi, Won‐,Kyoung,Park, Jin‐,Hun,Kim, Eun Jung,Cho, Jung‐,Hyuck,Ha, Hyun‐,Joon,Choi, Tae Hyun,Oh, Chang‐,Hyun John Wiley Sons, Ltd. 2011 Journal of labelled compounds & radiopharmaceutica Vol.54 No.2
<P><B>Abstract</B></P><P>Synthesis, radiolabelling, and <I>in vitro</I> evaluation of a new <SUP>125</SUP>I‐labelled iodouracil hexitol nucleoside analogue are reported. The target compound was successfully synthesized by an iodination–destannylation method and then purified by reverse phase HPLC. The radiochemical purity of the product was >99% with decay‐corrected yields of 48±3%. <I>In vitro</I> cellular uptake testing was carried out using MCA and MCA‐tk cell lines for comparison of compound 1 with [<SUP>18</SUP>F]FHBG. The newly synthesized compound 1 showed higher accumulation in herpex simplex virus type 1 thymidine kinase (HSV1‐tk) gene expression cell line (MCA‐tk cell line) than in the wild type MCA cell line compared with [<SUP>18</SUP>F]FHBG. The MCA‐tk to MCA cellular uptake ratio for compound 1 was higher than that of [<SUP>18</SUP>F]FHBG from 2 h after incubation. The radioiodine‐labelled compound 1 (I‐125, <I>t</I><SUB>1/2</SUB>=59.37 days) has a longer physical half‐life than F‐18‐(<I>t</I><SUB>1/2</SUB>=110 min) labelled FHBG. Radioiodine‐labelled compound 1 could be used for monitoring gene expression for a long time. The selectivity for MCA‐tk cell line makes compound 1 a promising imaging agent for HSV1‐tk expression. Copyright © 2010 John Wiley & Sons, Ltd.</P>
Design and Synthesis of an Anticancer Diarylurea Derivative with Multiple-Kinase Inhibitory Effect
Mohammed I. El-Gamal,오창현 대한화학회 2012 Bulletin of the Korean Chemical Society Vol.33 No.5
A diarylurea compound 1 possessing pyrrolo[3,2-c]pyridine nucleus was designed and synthesized with structure similarity to Sorafenib. Compound 1 was tested over 60-cancer cell line panel at a single dose concentration of 10 μM and showed high activity. It was further tested in a five-dose mode to determine its IC50, TGI, and LC50 values over the 60 cell lines. Compound 1 showed high potency and good efficacy, and was accordingly tested at a single dose concentration of 10 μM over a panel of 40 kinases. At this concentration, it completely inhibited the enzymatic activities of a number of oncogenic kinases, including ABL, ALK, c-RAF, FLT3, KDR, and TrkB. The target compound was subsequently tested over these 6 kinases in 10-dose testing mode in order to determine its IC50 values.
Mohammed I. El-Gamal,백대진,오창현 대한화학회 2016 Bulletin of the Korean Chemical Society Vol.37 No.2
In this paper, we report the synthesis of 14 new cycloalkane-fused tricyclic coumarin sulfonate derivatives. They were examined for in vitro anticancer activity against NCI-57 cancer cell line panel of nine different cancer types. Among all the target analogs, compounds 1c, 1e, and 1n showed the highest activities. Compound 1e exerted the highest percentage growth inhibition (91.91%) against SNB-75 CNS cancer cell line at 10 μM concentration and was more active than carmustine against this cell line. Compound 1c also showed strong activity against HT29 colon, ACHN renal, and PC-3 prostate cancer cell lines. Furthermore, compound 1n was selective toward the HT29 colon cancer cell line. Compounds 1c, 1e, and 1n showed superior selectivity against cancer cell lines compared to the noncancerous RAW 264.7 macrophages. The in silico predictions estimate the oral bioavailability, which is in compliance with Lipinski's rule of five.
Design and Synthesis of an Anticancer Diarylurea Derivative with Multiple-Kinase Inhibitory Effect
El-Gamal, Mohammed I.,Oh, Chang-Hyun Korean Chemical Society 2012 Bulletin of the Korean Chemical Society Vol.33 No.5
A diarylurea compound 1 possessing pyrrolo[3,2-$c$]pyridine nucleus was designed and synthesized with structure similarity to Sorafenib. Compound 1 was tested over 60-cancer cell line panel at a single dose concentration of 10 ${\mu}M$ and showed high activity. It was further tested in a five-dose mode to determine its $IC_{50}$, TGI, and $LC_{50}$ values over the 60 cell lines. Compound 1 showed high potency and good efficacy, and was accordingly tested at a single dose concentration of 10 ${\mu}M$ over a panel of 40 kinases. At this concentration, it completely inhibited the enzymatic activities of a number of oncogenic kinases, including ABL, ALK, c-RAF, FLT3, KDR, and TrkB. The target compound was subsequently tested over these 6 kinases in 10-dose testing mode in order to determine its $IC_{50}$ values.
El-Gamal, Mohammed I.,Oh, Chang-Hyun Korean Chemical Society 2011 Bulletin of the Korean Chemical Society Vol.32 No.3
Design and synthesis of new 3,4-diarylpyrazole-1-carboxamide derivatives are described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the diarylpyrazole scaffold was investigated. The pharmacological results indicated that most of the synthesized compounds showed moderate activity against A375, compared with Sorafenib. On the other hand, compounds Ia, Ie, IIb, and IIh were more potent than Sorafenib. In addition, compound IIa was equipotent to Sorafenib. Among all of these derivatives, compound IIb which has diethylamino and phenolic moieties showed the most potent antiproliferative activity against A375 human melanoma cell line. Virtual screening was carried out through docking of the most potent compound IIb into the domain of V600E-b-Raf and the binding mode was studied.
Mohammed I. El-Gamal,Chang-Hyun Oh 대한화학회 2011 Bulletin of the Korean Chemical Society Vol.32 No.3
Design and synthesis of new 3,4-diarylpyrazole-1-carboxamide derivatives are described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the diarylpyrazole scaffold was investigated. The pharmacological results indicated that most of the synthesized compounds showed moderate activity against A375, compared with Sorafenib. On the other hand, compounds Ia, Ie, IIb,and IIh were more potent than Sorafenib. In addition, compound IIa was equipotent to Sorafenib. Among all of these derivatives, compound IIb which has diethylamino and phenolic moieties showed the most potent antiproliferative activity against A375 human melanoma cell line. Virtual screening was carried out through docking of the most potent compound IIb into the domain of V600E-b-Raf and the binding mode was studied.
김현진,Mohammed I. El-Gamal,이용섭,오창현 대한화학회 2013 Bulletin of the Korean Chemical Society Vol.34 No.8
A new series of diarylamides and diarylureas having 2,3-dihydropyrrolo[3,2-b]quinoline scaffold was synthesized. Their in vitro antiproliferative activities were tested over NCI-60 cancer cell lines of nine different cancer types. Some target compounds showed good inhibition percentages over different cell lines. Among all the target compounds, compound 1f possessing 6,7-dimethoxy-2,3-dihydropyrrolo[3,2-b]quinoline nucleus, amide linker, and 4-chloro-3-(trifluoromethyl)phenyl terminal ring showed high selectivity against MCF7 and MDAMB- 468 breast cancer cell lines more than the other tested cell lines. Its inhibition percentages at 10 μM concentration over those two cell lines were 84.97% and 87.13%, respectively.
Radiosynthesis and Biodistribution of an 125I-labeled Resveratrol Derivative
Sung Kew Kim,Woong San Lee,Sang-Jin Han,Eun-Jung Kim,Mohammed I. El-Gamal,김병수,최태현,Chang Woon Choi,In-hye Ham,오창현,Ho-Young Choi,Jung-Hyuck Cho 대한화학회 2012 Bulletin of the Korean Chemical Society Vol.33 No.2
An 125I-labeled resveratrol derivative 1 was synthesized. It was purified by reverse phase HPLC. Radiochemical purity of the product was more than 98%, and the yield was 35% (decay-corrected). Its biodistribution in tumorbearing mice was studied. The results showed that the highest radioactivity was located in intestine and stomach. The biodistribution profile suggests that compound 1 can be effectively used as a promising imaging probe for intestine and stomach.
Amgad I. M. Khedr,Sabrin R. M. Ibrahim,Gamal A. Mohamed,Hany E. A. Ahmed,Amany S. Ahmad,Mahmoud A. Ramadan,Atef E. Abd El-Baky,Koji Yamada,Samir A. Ross 대한약학회 2016 Archives of Pharmacal Research Vol.39 No.7
Phytochemical investigation of Ficus pandurataHance (Moraceae) fruits has led to the isolation of two newtriterpenoids, ficupanduratin A [1b-hydroxy-3b-acetoxy-11a-methoxy-urs-12-ene] (11) and ficupanduratin B [21ahydroxy-3b-acetoxy-11a-methoxy-urs-12-ene] (17), alongwith 20 known compounds: a-amyrin acetate (1), a-amyrin(2), 3b-acetoxy-20-taraxasten-22-one (3), 3b-acetoxy-11amethoxy-olean-12-ene (4), 3b-acetoxy-11a-methoxy-12-ursene (5), 11-oxo-a-amyrin acetate (6), 11-oxo-b-amyrinacetate (7), palmitic acid (8), stigmast-4,22-diene-3,6-dione(9), stigmast-4-ene-3,6-dione (10), stigmasterol (12), b-sitosterol(13), stigmast-22-ene-3,6-dione (14), stigmastane-3,6-dione (15), 3b,21b-dihydroxy-11a-methoxy-olean-12-ene (16), 3b-hydroxy-11a-methoxyurs-12-ene (18), 6-hydroxystigmast-4,22-diene-3-one (19), 6-hydroxystigmast-4-ene-3-one (20), 11a,21a-dihydroxy-3b-acetoxy-urs-12-ene(21), and b-sitosterol-3-O-b-D-glucopyranoside (22). Compound21 is reported for the first time from a natural source. The structures of the 20 compounds were elucidated on thebasis of IR, 1D (1H and 13C), 2D (1H–1H COSY, HSQC,HMBC and NOESY) NMR and MS spectroscopic data, inaddition to comparison with literature data. The isolatedcompounds were evaluated for their anti-microbial, antimalarial,anti-leishmanial, and cytotoxic activities. In addition,their radioligand displacement affinity on opioid andcannabinoid receptors was assessed. Compounds 4, 11, and15 exhibited good affinity towards the CB2 receptor, withdisplacement values of 69.7, 62.5 and 86.5 %, respectively. Furthermore, the binding mode of the active compounds inthe active site of the CB2 cannabinoid receptors was investigatedthrough molecular modelling.