Synthetically modified methoxsalen for enhanced cytotoxicity in light and dark reactions.

Published on Feb 15, 2019in Bioorganic & Medicinal Chemistry Letters2.572
· DOI :10.1016/J.BMCL.2018.12.048
Christophe Guillon8
Estimated H-index: 8
(Lehigh University),
Yi-Hua Jan8
Estimated H-index: 8
(RU: Rutgers University)
+ 4 AuthorsNed D. Heindel20
Estimated H-index: 20
(Lehigh University)
Sources
Abstract
Abstract Linear furocoumarins, also known as psoralens, are clinically useful photo-activated pharmaceuticals employed to address hyperproliferative skin diseases. Seven diverse cytotoxic pharmacophores have been synthetically attached to 8-methoxypsoralen via a 5-amino functionality. The resulting unique set of compounds was evaluated for dark and light toxicity against PAM212 keratinocytes in culture.
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#1Paul T. Wilder (UMB: University of Maryland, Baltimore)H-Index: 22
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Cisplatin and other metal-based drugs often display side effects and tumor resistance after prolonged use. Because rhenium-based anticancer complexes are often less toxic, a novel series of organorhenium complexes were synthesized of the types: XRe(CO)3Z (X = α-diimines and Z = p-toluenesulfonate, 1-naphthalenesulfonate, 2-naphthalenesulfonate, picolinate, nicotinate, aspirinate, naproxenate, flufenamate, ibuprofenate, mefenamate, tolfenamate, N-acetyl-tryptophanate), and their biological proper...
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#1Jeffrey D. Laskin (RU: Rutgers University)H-Index: 69
#2Yi-Hua Jan (RU: Rutgers University)H-Index: 8
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: Photosensitizers are used in the treatment of epidermal proliferation and differentiation disorders such as psoriasis and vitiligo. In these studies, a ring-expanded carbon homolog of the linear psoralen (furo[3,2-g]benzopyran-7-one) class of photosensitizers, 4,10-dimethyl-2H,8H-benzo[1,2-b:5,4-b']dipyran-2-one (NDH2476), was synthesized and analyzed for biological activity. Following activation by ultraviolet light (UVA, 320-400 nm), NDH2476 was found to be a potent inhibitor of keratinocyte...
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AbstractPurpose: Melanoma is an aggressive form of skin cancer. The aim of the study was to evaluate the influence of UVA radiation and psoralens: 5-methoxypsoralen (5-MOP) or 8-methoxypsoralen (8-MOP) on melanoma cells viability.Materials and methods: The amelanotic C32 and melanotic COLO829 human melanoma cell lines were exposed to increasing concentrations of psoralens (0.1–100 μM) in the presence or absence of UVA radiation. Cell viability was evaluated by the WST-1 assay.Results: We demonst...
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Abstract A series of new antitumour lactones containing the [3.3.0] bicyclic furano-lactone core and the halogen or azido group at the C-7 position have been designed, synthesized, and evaluated for their in vitro antitumour activity against a panel of human tumour cell lines. Some of the analogues displayed powerful antiproliferative effects to certain human tumour cells, but all of them were devoid of any cytotoxicity towards the normal foetal lung fibroblasts (MRC-5). A SAR study reveals the ...
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