A silicon-containing aryl/penta-1,4-dien-3-one/amine hybrid exhibits antiproliferative effects on breast cancer cells by targeting the HSP90 C-terminus without inducing heat-shock response

Abstract

A pharmacophore-hybridized strategy based on the previously reported HSP90 C-terminal inhibitors was utilized to prepare 32 aryl/penta-1,4-dien-3-one/amine hybrids. Among them, a silicon-containing compound 1z exhibited remarkable broad-spectrum anti-proliferative effects on...

Biomimetic Total Synthesis of Bimagnolignan: A Natural Anti-Breast Cancer Agent

“…Previous study has shown that 1 exhibits a broad spectrum of in vitro antiproliferative activity against different human cancer cell lines, and driven by the continuous interests in the discovery of lead compounds for breast cancer treatment . We subjected seven derivatives of 1 , including 1a and 1b , as well as its stereoisomers (+)- 1 and (−)- 1 (resolved by chiral HPLC, see SI), and two other dimers 4a-1 (C–O coupling product) and 4b-1 (Scheme , details for these derivatives, see SI), to an in vitro antiproliferative activity screening in SKBr3 cells (Figure ).…”