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Synthesis and biological evaluation of pyrrole-based chalcones as CYP1 enzyme inhibitors, for possible prevention of cancer and overcoming cisplatin resistance
Inhibitors of CYP1 enzymes may play vital roles in the prevention of cancer and overcoming chemo-resistance to anticancer drugs. In this letter, we report synthesis of twenty-three pyrrole based heterocyclic chalcones ...
The synthesis of chalcones as anticancer prodrugs and their bioactivation in CYP1 expressing breast cancer cells
(Bentham Science Publishers, 2017-12-11)
Abstract: Background: Although the expression levels of many P450s differ between tumour and corresponding normal tissue, CYP1B1 is one of the few CYP subfamilies which is significantly and consistently overexpressed in ...
Identification of Potent and Selective CYP1A1 Inhibitors via Combined Ligand and Structure-Based Virtual Screening and Their in Vitro Validation in Sacchrosomes and Live Human Cells.
(ACS Publications, 2017-05-10)
Target structure-guided virtual screening (VS) is a versatile, powerful, and inexpensive alternative to experimental high-throughput screening (HTS). To discover potent CYP1A1 enzyme inhibitors for cancer chemoprevention, ...
Biotransformation of chrysin to baicalein: Selective C6- hydroxylation of 5,7-dihydroxyflavone using whole yeast cells stably expressing human CYP1A1 enzyme
(ACS Publications, 2017-08-07)
Naturally occurring polyphenolic compounds are of medicinal importance because of their unique antioxidant, anticancer and chemopreventive properties. Baicalein, a naturally occurring polyhydroxy flavonoid possessing ...