Synthesis and Antiproliferative Evaluation of Nitrofuranylvinylquinazolinone and Phenylpyrazole Derivatives

• Main Authors: Li-An Shih, 施俐安
• Other Authors: Yeh-Long Chen
• Format: Others
• Language: zh-TW
• Published: 2011
• Online Access: http://ndltd.ncl.edu.tw/handle/60953745249480431036

碩士 === 高雄醫學大學 === 醫藥暨應用化學研究所 === 99 === he thesis consists of two parts. Part A deals with the synthesis and antiproliferative evaluation of certain nitrofuranylvinylquinazolinone derivatives. Rational design of these nitrofuranylvinylquinazolinones is based on the published results in which nitrofuranylvinylquinolines have shown significant antiproliferactive activities while a series of quinazolinones were capable of inhibiting tubulin polymerization. Therefore, these newly synthesized nitrofuranylvinylquinazolinone derivatives can be considered as novel hybrid derivatives of nitrofuranylvinylquinolines and quinazolinones. Results indicated that certain newly synthesized nitrofuranylvinylquinazolinone derivatives exhibited potent antiproliferative activities. Part B deals with the synthesis and antiproliferative evaluation of certain chalcone derivatives which bears pyrazole ring. Chalcone derivatives have received considerable attention owing to their potent biological activities as anticancer and other agents. We have converted the ,??-methylene ketone group in chalcone pharmacophore into the pyrazole ring and to study the antiproliferative activities of these newly synthesized compounds. Result of antiproliferactive evaluation showed that these newly synthesized compounds exhibited better antiproliferative activities than their respective chalcone precursor.