Xu, Hongjiao published the artcileSynthesis and preliminary antitumor activity evaluation of 17-(5-(substituted cinnamamido)pentylamino)-17-demethoxygeldanamycin derivatives as potent Hsp90 Inhibitors, Recommanded Product: (E)-3-(3-Nitrophenyl)acrylic acid, the publication is Youji Huaxue (2015), 35(10), 2125-2134, database is CAplus.
Geldanamcyin (GA) was the first potent inhibitor of heat shock protein 90 (Hsp90) from natural products. However, its clin. application was limited by the unwanted hepatotoxicity. Our previous studies on the structure-activity relationships of GA derivatives indicated that the introduction of hepatoprotective cinnamoyl group via an alkyldiamino linker decreased the hepatotoxicity evidently. In this study, using pentyldiamine as the linker, twenty-six 17-(5-(substituted cinnamamido)pentylamino)-17-demethoxygeldanamycins were designed and synthesized as the inhibitors of Hsp90. All the compounds showed potent antitumor activities against human breast cancer cell line MDA-MB-231 with IC50 ranging from 0.12 to 1 ¦Ìmol¡¤L-1. Particularly, 17-(5-(cinnamamido)pentylamino)-17-demethoxygeldanamycin and 17-(5-(2,5-methoxycinn-amamido)pentylamino)-17-demethoxygeldanamycin were proved to be the most potent compounds (IC50 = 0.12 ¦Ìmol¡¤L-1), more active than the pos. control 17-N-allylamino-17-demethoxygeldanamycin (17-AAG) (IC50 = 0.27 ¦Ìmol¡¤L-1) and showed lower hepatotoxicity. Addnl., the preliminary structure-activity relationships among these newly synthesized congeners were briefly discussed, which should provide valuable basis for the structure optimization of GA-type Hsp90 inhibitors and antitumor lead compounds
Youji Huaxue published new progress about 1772-76-5. 1772-76-5 belongs to catalysis-chemistry, auxiliary class Benzenes, name is (E)-3-(3-Nitrophenyl)acrylic acid, and the molecular formula is C8H10S, Recommanded Product: (E)-3-(3-Nitrophenyl)acrylic acid.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia