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Mostafa M. Ghorab,Fatma A. Ragab,Helmy I. Heiba,Hebaallah M. Agha,Yassin M. Nissan 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.1
A series of novel 4-(4-substituted-thiazol-2-ylamino)-N-(pyridin-2-yl) benzene-sulfonamides were synthesized and screened for their cytotoxic activity against human breast cancer cell line (MCF-7). Compounds 6, 7, 9, 10, 11, and 14 displayed significant activity against MCF-7 when compared to doxorubicin, which was used as a reference drug. The synergistic effect of Gamma radiation for the most active derivatives 7, 9, and 11 was also studied and their IC50 values markedly decreased to 11.9 μM, 11.7 μM, and 11.6 μM, respectively.
Mostafa M. Ghorab,Zienab H. Ismail,Mohamad Abdalla,Awwad A. Radwan 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.6
A novel series of quinazolines 5–10, triazoloquinazolines11–17 and triazinoquinazoline 19 bearing abiologically active sulfonamide moiety were synthesized,utilizing methyl 2-isothiocyanato benzoate 2. Some of thenewly synthesized compounds revealed promising bacterialgrowth inhibition, compared with the ampicillin, as thereference drug. A LigandScout approach-generated pharmacophoremodel for the Staph aureus bacteria growthinhibition was done. The degree of fitting of the test setcompounds (3, 4, 6, 8, 11, 17) to the generated hypotheticalmodel revealed a qualitative measure of the more orless microbial inhibition of Staphylococcus aureus. Compounds(7, 8, 10, 12, 15, 17 and 22), which revealed significantactivity, are able to effectively satisfy the proposedpharmacophore geometry, using the energy accessibleconformers (Econf\20 kcal/mol).
Antitumor Activity of Novel Pyridine, Thiophene and Thiazole Derivatives
Mostafa M. Ghorab,Mansour S. Al-Said 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.6
2-Cyano-N'-[1-(2,5-dimethoxyphenyl)]ethylideneacetohydrazide 1 was obtained via reaction of cyanoacetic acid hydrazide with 2,5-dimethoxyacetophenone. A number of novel pyridines 2aj, 3, 4, thiophenes 5-9 and thiazoles 10-12 were prepared by using the hydrazide-hydrazone derivative 1 as a starting material. The structure of the newly synthesized compounds was characterized by elemental analyses, IR, 1H-NMR, 13C-NMR and mass spectral data. All the target compounds were subjected to in vitro antitumor activity against Ehrlich Ascites Carcinoma (EAC) cells. Compounds 2j and 6 showed a higher activity with IC50 values (54.54, 61.57 μM), 8 when compared with a reference drug IC50 value (68.99 μM), while compound 5 is nearly as active as Doxorubicin (CAS 23214-92-8).
Anticancer Activity of Novel Indenopyridine Derivatives
Mostafa M. Ghorab,Mansour S. Al-Said 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.6
Eighteen new 4-[2-amino-3-cyano-5-oxo-4-substitutedaryl-4H-indeno[1,2-b]pyridin-1-(5H)-yl]benzenesulfonamide derivatives 6a-q were synthesized via a reaction of aromatic aldehydes, enaminone 3 and malononitrile in one-pot reaction. Also, compounds 6a-q were obtained, via another route by reaction of enaminone 3 with arylidenemalononitriles 4a-q. The structure of the synthesized compounds was characterized by microanalysis, IR, 1H-NMR, 13C-NMR and mass spectral data. All the target compounds were subjected to in vitro anticancer activity against breast cancer cell line (MCF7). Compound 6d showed a higher potency with IC50 value (4.34 μM) than that of the Doxorubicin (5.40 μM), as the reference drug, while compound 6n with IC50 value (6.84 μM) is nearly as active as Doxorubicin. Also, compounds 6a-c, 6e, 6f, 6h and 6p exhibited a moderate activity, while compounds 3, 6g, 6i-m, 6o and 6q showed weak activity.
Mostafa M. Ghorab,Fatma A. Ragab,Helmi I. Heiba,Yassin M Nissan,Walid M. Ghorab 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.8
New quinoline derivatives 6, 7 and 19, pyrimidoquinoline derivatives 8-16 and triazolopyrimidoquinoline derivatives 17 and 18 bearing a bromo-substituent were synthesized starting from 3-(4-Bromophenylamino)-5,5-dimethylcyclohex-2-enone 3. All the newly synthesized compounds were evaluated for their in vitro anticancer activity against human breast cancer cell line (MCF7). Compounds 9, 11, 17 and 18 showed IC50 values (36.4, 39.7, 39.02 and 36.4 μM, respectively) comparable to that of the reference drug doxorubicin (IC50 = 32.02 μM). On the other hand, compound 6, 14 and 19 exhibited better activity than doxorubicin with IC50 values of 8.5, 23.5 and 23.7 μM. Additionally, the most potent compounds 6, 14 and 19 were evaluated for their ability to enhance the cell killing effect of γ-radiation.