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  • 02월 26일 17시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제115회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Novel 2,5-disubstituted quinolines: Design, synthesis, in-vitro antiproliferative activity and kinase profile

등록일
2015년 2월 27일 12시 52분 28초
접수번호
1526
발표코드
KCS2.O-2 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
목 09시 : 15분
발표형식
구두발표
발표분야
Oral Presentation for Young International Chemists
저자 및
공동저자
ELDAMASY ASHRAF KAREEM AWAD MOHAMMED, 강순방1, 금교창2,*
과학기술연합대학원대학교(UST) 생물화학, 한국과학기술연구원(KIST) 뇌의약연구단, Korea
1한국과학기술연구원(KIST) 뇌의약연구단, Korea
2한국과학기술연구원(KIST) 케모인포메틱스연구센터, Korea
Four novel series of 2,5-disubstituted quinolines (53 final compounds) have been designed and synthesized as anticancer sorafenib analogues. Two series (amides & ureas) were designed to possess a spacer between the terminal aryl and 2-aminoquinoline scaffold, whereas the other series (C & D) lack the spacer while conserving the oxypicolinamide or propoxy moiety at 5-position, respectively. All the target compounds were preliminary evaluated for their antiproliferative effect against three cancer cell lines (MCF7, HCT116 and SKBR3) by MTT assay and exhibited promising antitumor activity. Therefore, 35 compounds were selected to be tested over a panel of 60 cancer cell lines at a single dose concentration of 10 μM at NCI to broadly screen their antiproliferative activity. Fifteen compounds have showed promising mean growth inhibitions and thus were further tested at five-dose testing mode to determine their GI50, TGI and LC50 over the 60 cell lines. The data obtained revealed that KK9087 is the most potent and efficacious derivatives with submicromolar GI50 value against some cell lines. Furthermore, it was screened against a panel of 46 oncogenic kinases at single dose of 10 μM and showed selective high inhibition (96%) against TrKA with IC50 value of 2.5 μM, so it can be an attractive candidate for further investigatio

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