An article CYP enzymes, expressed within live human suspension cells, are superior to widely-used microsomal enzymes in identifying potent CYP1A1/CYP1B1 inhibitors: Identification of quinazolinones as CYP1A1/CYP1B1 inhibitors that efficiently reverse B[a] P toxicity and cisplatin resistance WOS:000460399800020 published article about HUMAN CYTOCHROME-P450 ENZYMES; IN-VITRO; CANCER-RISK; ESTROGEN METABOLISM; DRUG; HYDROXYLATION; POLYMORPHISM; DERIVATIVES; VALIDATION; INITIATION in [Sonawane, Vinay R.; Gatchie, Linda; Williams, Ibidapo S.; Chaudhuri, Bhabatosh] CYP Design Ltd, Innovat Ctr, 49 Oxford St, Leicester LE1 5XY, Leics, England; [Siddique, Mohd Usman Mohd; Jayaprakash, Venkatesan; Sinha, Barij N.] Birla Inst Technol, Dept Pharmaceut Sci & Technol, Ranchi 835215, Bihar, India; [Bharate, Sandip B.] CSIR Indian Inst Integrat Med, Med Chem Div, Cana Rd, Jammu 180001, Jammu & Kashmir, India in 2019, Cited 69. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6. SDS of cas: 88-68-6
Microsomal cytochrome P450 (CYP) enzymes, isolated from recombinant bacterial/insect/yeast cells, are extensively used for drug metabolism studies. However, they may not always portray how a developmental drug would behave in human cells with intact intracellular transport mechanisms. This study emphasizes the usefulness of human HEK293 kidney cells, grown in ‘suspension’ for expression of CYPs, in finding potent CYP1A1/CYP1B1 inhibitors, as possible anticancer agents. With live cell-based assays, quinazolinones 9i/9b were found to be selective CYP1A1/CYP1B1 inhibitors with IC50 values of 30/21 nM, and > 150-fold selectivity over CYP2/3 enzymes, whereas they were far less active using commercially-available CYP1A1/CYP1B1 microsomal enzymes (IC50, > 10/1.3-1.7 mu M). Compound 9i prevented CYP1A1-mediated benzo [a]pyrene-toxicity in normal fibroblasts whereas 9b completely reversed cisplatin resistance in PC-3/prostate, COR-L23/1ung, MIAPaCa-2/pancreatic and LS174T/colon cancer cells, underlining the human-cell-assays’ potential. Our results indicate that the most potent CYP1A1/CYP1B1 inhibitors would not have been identified if one had relied merely on microsomal enzymes.
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