Antineoplastic Constituents from the Chemical Diversified Extract of Radix puerariae. Issue 1 (28th December 2018)

• Record Type: Journal Article
• Authors: Zhang, Jian‐Long; Xu, Wei; Zhou, Zhen‐Ru; Li, Juan; Jiang, Lin‐Lin; Zhang, Xing‐Xiao; Jiang, Ren‐Wang
• Is Part Of: Chemistry & biodiversity. Volume 16:Issue 1(2019)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2018-12-28
• Subjects: Radix puerariae -- Pueraria montana var. lobatea -- semisynthetic -- antineoplastic activity -- biological activity -- natural products; Biochemistry -- Periodicals; Molecular biology -- Periodicals; Biodiversity -- Periodicals; 572
• DOI: 10.1002/cbdv.201800408
• Languages: English
• ISSNs: 1612-1872

Abstract

Abstract: To enhance the structural diversity of isoflavonoids and provide more derivatives for the biological screening, a semisynthetic mixture was generated by diversification of the crude extract of Radix puerariae ( Pueraria montana var . lobata ) through the chemical reaction with hydrazine hydrate. Eleven 3, 4‐diarylpyrazoles (1 –11 ) and two 5‐phenyl‐6‐benzyldihydropyridazinones (12 and13 ) were isolated from the semisynthetic mixture, and their structures were identified by spectroscopic methods in combination with X‐ray crystallographic analysis. Among them, nine compounds (5 –13 ) were new derivatives. All the compounds were evaluated on the inhibitory activities against the prostate cancer cell lines LNCaP and PC3. Compounds12 and13 were found to exhibit much more potent inhibitory activities against the androgen dependent LNCaP cells than the androgen independent PC3 cells. Rapid synthesis of new 3, 4‐diarylpyrazoles and two 5‐phenyl‐6‐benzyldihydropyridazinones with significant biological activity highlights the great potential of one‐pot combinatorial modification for the diversification of natural products. Abstract :