An article Psoralen Derivatives with Enhanced Potency WOS:000542397500001 published article about WAVELENGTH DEPENDENCE; FUROCOUMARIN DERIVATIVES; ACID PHOTOREACTION; CROSS-LINKING; DNA; 8-METHOXYPSORALEN; CELLS; PHOTOCHEMOTHERAPY; MONOADDUCTS; INHIBITION in [Buhimschi, Alexandru D.] Northwestern Univ, Feinberg Sch Med, Med Scientist Training Program, Chicago, IL 60611 USA; [Buhimschi, Alexandru D.; Gasparro, Francis P.] Hamden Hall Country Day Sch, Photobiol Lab, Hamden, CT 06517 USA; [Gooden, David M.] Duke Univ, Dept Chem, Durham, NC 27706 USA; [Jing, Hongwu] Univ Illinois, Coll Med, Dept Obstet & Gynecol, Chicago, IL 60612 USA; [Fels, Diane R.; Hansen, Katherine S.; Dewhirst, Mark W.] Duke Univ, Med Ctr, Dept Radiat Oncol, Durham, NC USA; [Fels, Diane R.; Hansen, Katherine S.; Dewhirst, Mark W.] Duke Univ, Med Ctr, Duke Canc Inst, Durham, NC USA; [Beyer, Wayne F., Jr.; Walder, Harold] Immunolight LLC, Detroit, MI USA in 2020.0, Cited 58.0. The Name is Diphenyl oxide. Through research, I have a further understanding and discovery of 101-84-8. Recommanded Product: Diphenyl oxide
Psoralen is a furocoumarin natural product that intercalates within DNA and forms covalent adducts when activated by ultraviolet radiation. It is well known that this property contributes to psoralen’s clinical efficacy in several disease contexts, which include vitiligo, psoriasis, graft-versus-host disease and cutaneous T-cell lymphoma. Given the therapeutic relevance of psoralen and its derivatives, we attempted to synthesize psoralens with even greater potency. In this study, we report a library of 73 novel psoralens, the largest collection of its kind. When screened for the ability to reduce cell proliferation, we identified two derivatives even more cytotoxic than 4 ‘-aminomethyl-4,5 ‘,8-trimethylpsoralen (AMT), one of the most potent psoralens identified to date. Using MALDI-TOF MS, we studied the DNA adduct formation for a subset of novel psoralens and found that in most cases enhanced DNA binding correlated well with cytotoxicity. Generally, our most potent derivatives contain positively charged substituents, which we believe increase DNA affinity and enhance psoralen intercalation. Thus, we provide a rational approach to guide efforts toward further optimizing psoralens to fully capitalize on this drug class’ therapeutic potential. Finally, the structure-activity insights we have gained shed light on several opportunities to study currently underappreciated aspects of psoralen’s mechanism.
About Diphenyl oxide, If you have any questions, you can contact Buhimschi, AD; Gooden, DM; Jing, HW; Fels, DR; Hansen, KS; Beyer, WF; Dewhirst, MW; Walder, H; Gasparro, FP or concate me.. Recommanded Product: Diphenyl oxide
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