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Azza T. Taher,Nadia A. Khalil,Eman M. Ahmed 대한약학회 2011 Archives of Pharmacal Research Vol.34 No.10
A series of new isatin-thiazoline 3a-h and isatin-benzimidazole 4a-h derivatives were synthesized via condensation of isatin Mannich bases 2a-h with either 2-aminothiazoline or 2-aminobenzimidazole. The structures of the newly synthesized compounds were characterized by spectral data. The anti-breast cancer activity of some of the synthesized compounds was assessed in the MCF-7 human breast cancer cell line. The results showed that compounds 4b, 4d and 4g possess significant antiproliferative activity against MCF-7 cells.
Azza T. Taher,Lamia W. Mohammed 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.6
New derivatives of 1,3,4-benzotriazepin-5-onewere designed and synthesized as structural analogues tothe antitumor agents devazepide and asperlicin. An efficientand novel approach to the synthesis of 2-amino-1,3,4-benzotriazepin-5-one 2 was developed and its structure wasconfirmed. The newly synthesized derivatives were evaluatedfor their in vitro antitumor activity on 60 differentcell lines. Compounds 8 and 9 displayed the most potentantitumor activity against several cell lines specificallyovarian cancer, renal cancer and prostate cancer, whilecompounds 5, 10 and 12 showed significant activitiesagainst UO-31 renal cancer cell line.
Synthesis of novel bis-anthraquinone derivatives and their biological evaluation as antitumor agents
Azza T. Taher,Gehan H. Hegazy 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.5
Cancer has become a major worldwide problemand drug resistance now is one of the most important problemsin treatment of cancer. Anthraquinone derivativesrepresent one of the most important drugs that can be used intreatment of many types of cancer. In this study two series ofnovel bis-anthraquinone derivatives have been synthesized. Five of these compounds were chosen to be evaluated fortheir antitumor activity against human cancer cell lines bythe National Cancer Institute (NCI, USA). Marked activitywas shown for the tested compounds(2–6). The most activeone was compound 6 with mean value-67.00 against all celllines. Compounds 7 and 8 were found inactive.
Salwa Elmeligie,Azza T. Taher,Nadia A. Khalil,Ahmed H. El-said 대한약학회 2017 Archives of Pharmacal Research Vol.40 No.1
Novel series of 1,3,4-trisubstituted azetidin-2-one derivatives 8a–p were synthesized and proposed ascytotoxic agents acting via inhibition of tubulin at thecolchicine binding site. The design of the target compoundswas based upon modification in the structure of the vasculartargeting agent combretastatin A-4 (CA-4). The cisdouble bond linker in CA-4 was replaced with the azetidin-2-one ring aiming to prevent the cis/trans isomerizationthat suppresses the activity of CA-4, thereby enhancing itsantiproliferative activity. All new compounds were investigatedin vitro against MCF-7 and HCT-116 cell lines. Theinhibition of tubulin polymerization by four most potentcompounds 8g, 8j, 8n and 8o was also evaluated. Thesynthesis of the final targets was achieved adopting Staudingerreaction. Molecular modeling studies were performedto rationalize the biological results.