160893-07-2Relevant articles and documents
Design and synthesis of new 2-anilinoquinolines bearing N-methylpicolinamide moiety as potential antiproliferative agents
El-Damasy, Ashraf Kareem,Seo, Seon Hee,Cho, Nam-Chul,Pae, Ae Nim,Kim, Eunice Eunkyeong,Keum, Gyochang
, p. 98 - 113 (2017)
A series of new 2-anilinoquinolines 6a–o possessing the substantial N-methylpicolinamide motif at C5 has been designed and synthesized as sorafenib analogs. The antiproliferative activities of the target compounds were preliminarily appraised against a panel of three human cancer cell lines (MCF-7, SK-BR3, and HCT116), and a selected array was further tested over a panel of approximately 60 cancer cell lines at NCI at 10?μM concentration. Interestingly, compounds 6c, 6d, 6j, 6k, and 6l showed promising selective anticancer activities (growth inhibition >80%) toward certain cancer cells at 10?μM testing dose. Compounds 6d and 6j were advanced to five-dose testing mode to determine their GI50 values and compared with our previously reported ureidoquinoline B and sorafenib as reference compounds. The 4-chloro-3-trifluoromethylaniline derivative 6j manifested superior potency than both compound B and sorafenib over eleven and eight cell lines, respectively. It showed GI50 values of 0.36, 0.66, 0.68, and 0.60?μM against the breast MDA-MB-468, renal A498, and melanoma SK-MEL-5 and UACC-62 cell lines, respectively. Moreover, both 6d and 6j exerted low cytotoxic effects against HFF-1 normal cell line. Furthermore, compounds 6d and 6j were tested against both B-RafV600E and C-Raf kinases and displayed modest inhibitory activities, which were justified by molecular docking study. Compound 6j could serve as a promising candidate for further development of potent anticancer chemotherapeutics.
NOVEL QUINOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS FOR PREVENTING OR TREATING CANCER CONTAINING THE SAME
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, (2017/11/10)
The present invention refers to an excellent cancer antiproliferative potency relative to the quinoline compounds, a pharmaceutically acceptable salt, or hydrate and, number of active ingredient containing bath method and pharmaceutical composition for the prevention or treatment of cancer disease relates to search, said present invention according to compound, a pharmaceutically acceptable salt thereof, or hydrate number and number and mutant kinase protein kinase activity number of excellent cancer billion billion number activity and thus, new anticancer number is useful as the effective component can be. (by machine translation)
Design, synthesis, in-vitro antiproliferative activity and kinase profile of new picolinamide based 2-amido and ureido quinoline derivatives
El-Damasy, Ashraf Kareem,Seo, Seon Hee,Cho, Nam-Chul,Kang, Soon Bang,Pae, Ae Nim,Kim, Key-Sun,Keum, Gyochang
, p. 754 - 768 (2015/08/06)
Abstract New 2-amido and ureido quinoline derivatives substituted with 2-N-methylamido-pyridin-4-yloxy group at the 5-position of quinoline (18 final compounds) have been designed and synthesized as anticancer sorafenib congeners. Among the synthesized de