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Synthesis of α-santonin Derivatives for Diminutive Effect on T and B-cell Proliferation and Their Structure Activity Relationships

Synthesis of α-santonin Derivatives for Diminutive Effect on T and B-cell Proliferation and Their Structure Activity Relationships

Praveen K Chinthakindi, Jasvinder Singh, Shilpa Gupta, Amit Nargotra, Priya Mahajan, Anupurna Kaul, Zabeer Ahmed, Surrinder Koul, Payare L Sangwan

Eur J Med Chem. 2017 Feb 15;127:1047-1058.

PMID: 27847171

Abstract:

A new library of 20 compounds from α-santonin was synthesized and tested against Con-A induced T-cell proliferation and LPS-induced B-cell proliferation via MTT assay. The study resulted in the identification of potent immunosuppressant molecules, which were further screened along with α-santonin for Tumor Necrosis Factor Alpha (TNF-α) inhibitory activity. One of the molecules (7) at 10 μM showed equipotency to that of dexamethasone (1 μM conc.) used as a standard. Structure activity relationships of the synthesized compounds along with our earlier reported α-santonin derivatives have been studied. Inferences from the modifications carried out at all the three sites of α-santonin have been elaborated. Computational study of the active compounds shows TNF-α protein as its preferable target rather than Inosine Monophosphate Dehydrogenase (IMPDH).

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP481061	α-Santonin		481-06-1	Price

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