Sparsomycin Analogs. IV. : Synthesis and Antitumor Activity of Pyrimidine-5-carboxamides and (E)-β-(Pyrimidin-5-yl)-acrylamides
-
- KANATOMO SHOICHI
- School of Pharmacy, Hokuriku University
-
- WADA AKIMORI
- School of Pharmacy, Hokuriku University
-
- YOMEI MASAKATSU
- School of Pharmacy, Hokuriku University
-
- HASE TETSUKO
- School of Pharmacy, Hokuriku University
-
- NAGAI SOTOO
- School of Pharmacy, Hokuriku University
-
- FUKUDA SHIZUO
- School of Pharmacy, Hokuriku University
-
- TANAKA MOTOHIRO
- Japan and Chemotherapy Division, National Cancer Center Research Institute
-
- SASAKI TAKUMA
- Japan and Chemotherapy Division, National Cancer Center Research Institute
Search this article
Description
Various pyrimidine-5-carboxamides (14,16,18,20,and 21) and (E)-β-(pyrimidin-5-yl)acrylamides (15,17,19,and 22)were synthesized as sparsomycin analogs, and their antitumor activity was examined by cell growth inhibition assay against mouse leukemia L5178Y cells in vitro.Synthesis was carried out by condensation of appropriate acids (4,6,10,and 12) and amino acid methyl esters (13) by the mixed anhydride method using isobutyl chlorocarbonate. The condensation product was converted to the corresponding acid and alcohol derivatives by hydrolysis and LiBH_4 reduction. The compounds having an ethylene linkage at the C-5 position and an ester moiety at the terminal amino acid functionality (15b, and 17b-g) exhibited remarkable antitumor activity.
Journal
-
- Chemical & pharmaceutical bulletin
-
Chemical & pharmaceutical bulletin 36 (6), 2042-2049, 1988-06-25
The Pharmaceutical Society of Japan
- Tweet
Keywords
Details 詳細情報について
-
- CRID
- 1572824502321224960
-
- NII Article ID
- 110003627034
-
- NII Book ID
- AA00602100
-
- ISSN
- 00092363
-
- Text Lang
- en
-
- Data Source
-
- CiNii Articles