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1
Synthesis of α-santonin derived acetyl santonous acid triazole derivatives and their bioevaluation for T and B-cell proliferation.α-山道年衍生的乙酰山道年酸三唑衍生物的合成及其对T细胞和B细胞增殖的生物学评价。
Eur J Med Chem. 2016 Sep 14;120:160-9. doi: 10.1016/j.ejmech.2016.05.018. Epub 2016 May 10.
2
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J Nat Prod. 2016 Mar 25;79(3):629-61. doi: 10.1021/acs.jnatprod.5b01055. Epub 2016 Feb 7.
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Eur J Med Chem. 2016 Jan 27;108:104-116. doi: 10.1016/j.ejmech.2015.11.018. Epub 2015 Nov 19.
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New horizons for old drugs and drug leads.老药和先导药物的新视野。
J Nat Prod. 2014 Mar 28;77(3):703-23. doi: 10.1021/np5000796. Epub 2014 Feb 5.
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Synthesis of 3-O-propargylated betulinic acid and its 1,2,3-triazoles as potential apoptotic agents.3-O-丙炔基白桦酸及其 1,2,3-三唑衍生物的合成及其作为潜在凋亡试剂的研究。
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Synthesis and anticancer activity of novel spiro-isoxazoline and spiro-isoxazolidine derivatives of α-santonin.新型α-山道年螺环异恶唑啉和螺环异恶唑烷衍生物的合成及抗癌活性。
Eur J Med Chem. 2013 May;63:279-89. doi: 10.1016/j.ejmech.2013.01.003. Epub 2013 Jan 11.
7
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新型α-山道年类似物对Balb/c小鼠体液和细胞免疫反应的T细胞和B细胞免疫抑制活性

T- and B-cell immunosuppressive activity of novel α-santonin analogs with humoral and cellular immune response in Balb/c mice.

作者信息

Dangroo Nisar A, Singh Jasvinder, Gupta Nidhi, Singh Shashank, Kaul Anapurna, Khuroo Mohmmed A, Sangwan Payare L

机构信息

Bioorganic Chemistry Division , Canal Road , Jammu-180001 , India.

Cancer Pharmacology Division , CSIR-Indian Institute of Integrative Medicine , Canal Road , Jammu-180001 , India.

出版信息

Medchemcomm. 2016 Nov 11;8(1):211-219. doi: 10.1039/c6md00527f. eCollection 2017 Jan 1.

DOI:10.1039/c6md00527f
PMID:30108707
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6072515/
Abstract

In continuation of our endeavours to synthesize immunosuppressive agents from α-santonin, we report herein the design and synthesis of a new series of α-santonin derived O-aryl/aliphatic ether, ester and amide analogs and the evaluation of their immunosuppressive activities. The studies led to several analogs with significant immunosuppressive effects by inhibiting ConA and LPS stimulated T- and B-cell proliferation in a dose dependent manner. The more significant compounds , , , , and displayed potent inhibitory activity on the mitogen-induced T- and B-cell proliferation in comparison to α-santonin . Compound displayed stupendous immunosuppressive effects with ∼80% suppression of B and ∼75% suppression of T lymphocyte proliferation, respectively The investigation on BALB/c mice revealed that non-cytotoxic compound suppresses both humoral and cellular immunity.

摘要

在我们继续努力从α-山道年合成免疫抑制剂的过程中，本文报道了一系列新的α-山道年衍生的O-芳基/脂肪族醚、酯和酰胺类似物的设计与合成及其免疫抑制活性评估。这些研究得到了几种具有显著免疫抑制作用的类似物，它们通过剂量依赖性方式抑制刀豆蛋白A（ConA）和脂多糖（LPS）刺激的T细胞和B细胞增殖。与α-山道年相比，更具活性的化合物 、 、 、 、 和 对有丝分裂原诱导的T细胞和B细胞增殖表现出强大的抑制活性。化合物 表现出惊人的免疫抑制作用，分别对B淋巴细胞增殖有80%的抑制率，对T淋巴细胞增殖有75%的抑制率。对BALB/c小鼠的研究表明，无细胞毒性的化合物 可抑制体液免疫和细胞免疫。